Search Result
Results for "
EGFR+tyrosine+kinase
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
17
Isotope-Labeled Compounds
| Art. -Nr. |
Produktname |
Target |
Forschungsgebiete |
Chemical Structure |
-
- HY-50895
-
Gefitinib
Maximum Cited Publications
200 Publications Verification
ZD1839
|
EGFR
Autophagy
Apoptosis
|
Cancer
|
|
Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .
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-
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- HY-50896
-
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CP-358774; NSC 718781; OSI-774
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EGFR
Autophagy
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Cancer
|
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Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer . Erlotinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
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- HY-50898
-
-
-
- HY-13524
-
-
-
- HY-148810
-
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BI 1810631
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c-Met/HGFR
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Cancer
|
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Zongertinib (BI 1810631) is a potent and selective HER2 and EGFR tyrosine kinase inhibitor with IC50 values of 13 nM and 579 nM, respectively. Zongertinib has antitumor activity and can be used in the study of multiple solid tumors .
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-
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- HY-112823
-
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HS-10296
|
EGFR
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Cancer
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Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
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-
-
- HY-19730
-
|
HM61713; BI 1482694
|
EGFR
|
Cancer
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Olmutinib (HM61713; BI-1482694) is an orally active and irreversible third EGFR tyrosine kinase inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib is used for NSCLC .
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-
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- HY-112299
-
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TAS6417; CLN-081
|
EGFR
Apoptosis
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Cancer
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Zipalertinib (TAS6417; CLN-081) is a highly effective, orally active and pan-mutation-selective EGFR tyrosine kinase inhibitor with a unique scaffold fitting into the ATP-binding site of the EGFR hinge region, with IC50 values ranging from 1.1-8.0 nM .
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-
-
- HY-50898A
-
-
-
- HY-50895A
-
|
ZD-1839 hydrochloride
|
EGFR
|
Cancer
|
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Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib hydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib hydrochloride also induces autophagy. Gefitinib hydrochloride has antitumour activity .
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-
- HY-129550
-
|
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EGFR
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Cancer
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BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor. BI-4020 inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM). BI-4020 also shows activity against EGFR wt (IC50=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties .
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-
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- HY-50898B
-
|
GW572016 ditosylate monohydrate; GW2016 ditosylate monohydrate
|
EGFR
Autophagy
Ferroptosis
|
Infection
Metabolic Disease
Cancer
|
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Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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-
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- HY-10322
-
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BIBX 1382
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EGFR
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Cancer
|
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Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity .
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- HY-144680
-
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ZL-2313
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EGFR
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Cancer
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BLU-945 is a potent, highly selective, reversible and orally active epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKIs). BLU-945 can effectively inhibit EGFR with L858R and/or exon 19 deletion mutation, T790M mutation and C797S mutation. BLU-945 can be used for the research of lung cancer including non-small cell lung cancer (NSCLC) .
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- HY-117155
-
PKI-166
1 Publications Verification
|
EGFR
|
Cancer
|
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PKI-166 is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM .
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- HY-50896R
-
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CP-358774 (Standard); NSC 718781 (Standard); OSI-774 (Standard)
|
Reference Standards
EGFR
Autophagy
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Cancer
|
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Erlotinib (Standard) is the analytical standard of Erlotinib. This product is intended for research and analytical applications. Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer . Erlotinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-136430
-
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JGK037
|
EGFR
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Cancer
|
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JCN037 (JGK037) is non-covalent and BBB-penetrant EGFR tyrosine kinase inhibitor, with IC50 values of 2.49 nM, 3.95 nM, 4.48 nM for EGFR, p-wtEGFR and pEGFRvⅢ, respectively .
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-
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- HY-13896
-
|
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EGFR
Autophagy
Apoptosis
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Cancer
|
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PD168393 is a potent, selective and cell-permeable inhibitor of EGFR tyrosine kinase and ErbB2. PD168393 irreversiblely inactivates EGF receptor ( IC50=0.7 nM) and is inactive against insulin receptor, PDGFR, FGFR and PKC .
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- HY-109189
-
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BPI-7711
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EGFR
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Cancer
|
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Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity .
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-
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- HY-112823B
-
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HS-10296 hydrochloride
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EGFR
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Cancer
|
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Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer .
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-
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- HY-112823A
-
|
HS-10296 mesylate
|
EGFR
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Cancer
|
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Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib mesylate is used for the research of the non-small cell lung cancer .
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- HY-18963
-
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RG-14355
|
EGFR
|
Cancer
|
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Lavendustin A (RG-14355) is a potent, selective and ATP-competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, with an IC50 of 11 nM. Lavendustin A does not inhibit protein kinase A or C. Lavendustin A can suppress VEGF-induced angiogenesis .
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- HY-139300
-
|
HMPL-813
|
EGFR
|
Cancer
|
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Epitinib (HMPL-813) is a selective, orally active, blood-brain barrier-permeable EGFR tyrosine kinase inhibitor. Epitinib is applicable to research on EGFR T790M-positive non-small cell lung cancer with brain metastasis and advanced solid tumors .
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- HY-12972
-
|
PF-06747775
|
EGFR
|
Cancer
|
|
Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC) .
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-
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- HY-101042
-
|
Tyrphostin AG 494
|
EGFR
CDK
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Cancer
|
|
AG-494 (Tyrphostin AG 494) is a potent and selective EGFR tyrosine kinase inhibitor (IC50=0.7 μM). AG-494 inhibits the autophosphorylation of EGFR, ErbB2, HER1-2 and PDGF-R with IC50s 1.1, 39, 45 and 6 μM, respectively. AG-494 blocks Cdk2 activation and inhibits EGF-dependent DNA synthesis .
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- HY-108484
-
|
|
EGFR
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Cancer
|
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PP 3 (Compound 3) is an EGFR tyrosine kinase inhibitor with an IC50 of 2.7 μM .
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- HY-101820
-
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EGFR
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Cancer
|
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Simotinib is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities .
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- HY-131088
-
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Drug-Linker Conjugates for ADC
EGFR
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Cancer
|
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N3-PEG8-Phe-Lys-PABC-Gefitinib is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-tumor agent, Gefitinib (HY-50895) (orally active EGFR tyrosine kinase inhibitor), linked via the cleavable linker N3-PEG8-Phe-Lys-PABC. N3-PEG8-Phe-Lys-PABC-Gefitinib is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-12806
-
|
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EGFR
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Cancer
|
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AG1557 is a specific and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, has a pIC50 value of 8.194 .
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- HY-118532
-
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AG30
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EGFR
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Cancer
|
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Tyrphostin AG30 (AG30) is a potent and selective EGFR tyrosine kinase inhibitor. Tyrphostin AG30 (AG30) selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in primary erythroblasts .
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- HY-50898S4
-
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GW572016-d7; GW2016-d7
|
Isotope-Labeled Compounds
Autophagy
EGFR
Ferroptosis
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Cancer
|
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Lapatinib-d7 (GW572016-d7) is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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-
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- HY-50896S
-
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CP-358774-d6; NSC 718781-d6; OSI-774-d6
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EGFR
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Cancer
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Erlotinib-d6 (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR . Erlotinib-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
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- HY-50895R
-
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ZD1839 (Standard)
|
Reference Standards
EGFR
Autophagy
Apoptosis
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Cancer
|
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Gefitinib (Standard) is the analytical standard of Gefitinib. This product is intended for research and analytical applications. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .
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- HY-15772S3
-
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asandeutertinibum; Osimertinib-d3; AZD-9291-d3
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EGFR
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Cancer
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Asandeutertinib (Osimertinib-d3; AZD-9291-d3) is a epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, with antineoplastic effect .
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- HY-133779
-
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Drug Metabolite
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Cancer
|
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Gefitinib impurity 5 is the impurity of Gefitinib (HY-133779). Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces Autophagy. Gefitinib has antitumour activity .
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- HY-50895S2
-
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Isotope-Labeled Compounds
EGFR
Autophagy
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Cancer
|
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Gefitinib-d3 (ZD1839-d3) is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity .
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- HY-101958
-
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AG82; Tyrphostin A 25; Tyrphostin AG 82; RG-50875
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EGFR
GPR35
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Inflammation/Immunology
Cancer
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Tyrphostin 25 (AG82) is a specific inhibitor of the EGFR tyrosine kinase with an IC50 value of 3 µM in A431 cells. Tyrphostin 25 is also a GPR35 agonist with an EC50 of 5.3 µM .
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- HY-13524A
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-
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- HY-148871
-
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Drug-Linker Conjugates for ADC
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Cancer
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Mc-Val-Cit-PAB-Gefitinib chloride is a agent-linker conjugates for ADC. Mc-Val-Cit-PAB-Gefitinib chloride consists of Gefitinib (HY-50895) (an EGFR tyrosine kinase inhibitor) and the ADC linker Mc-Val-Cit-PAB .
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-
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- HY-50895G
-
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ZD1839
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EGFR
Autophagy
Apoptosis
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Cancer
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Gefitinib (ZD1839) (GMP) is Gefitinib (HY-50895) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Gefitinib is a potent, selective and orally active EGFR tyrosine kinase inhibitor .
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-
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- HY-50898S1
-
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GW572016-d7 dihydrochloride; GW2016-d7 dihydrochloride
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Isotope-Labeled Compounds
EGFR
Autophagy
Ferroptosis
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Cancer
|
|
Lapatinib-d7 dihydrochloride is the deuterium labeled Lapatinib dihydrochloride. Lapatinib (GW572016) dihydrochloride is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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-
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- HY-50898S
-
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GW572016-d4; GW2016-d4
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EGFR
Autophagy
Ferroptosis
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Cancer
|
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Lapatinib-d4 is the deuterium labeled Lapatinib (HY-50898). Lapatinib is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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- HY-117852
-
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TRX-13
|
EGFR
Tyrosinase
|
Cancer
|
|
CGP-59326 (TRX-13) is a highly potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (IC50=0.027 μM). CGP-59326 blocks the EGFR signaling pathwa, demonstrating highly selective inhibition of EGFR-dependent tumor cells. CGP-59326 is promising for research of cancers .
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-
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- HY-N12726
-
|
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p38 MAPK
MMP
|
Infection
Inflammation/Immunology
Cancer
|
Halociline, a derivative of alkaloids, that can be isolated from the marine fungus Penicillium griseofulvum.
Halociline targets MAPK1, MMP-9, and PIK3CA in gastric cancer cells, potentially mediated by diverse pathways including cancer, lipid metabolism, atherosclerosis, and EGFR tyrosine kinase inhibitor resistance. Halociline possesses antimicrobial, antioxidant and biofilm inhibitory activities .
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- HY-156741A
-
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EGFR
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Cancer
|
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EGFR-IN-87 (Compound Example 2) hydrochloride is a EGFR tyrosine kinase inhibitor. EGFR-IN-87 hydrochloride has IC50 value of 3.1 nM, 1.3 nM and 7.1 nM for EGFR_d746-750, EGFR_L858R/T790 and EGFR_WT in A431 cells, respectively. EGFR-IN-87 hydrochloride can be used for cancer diseases research .
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-
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- HY-129510
-
|
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EGFR
Mitosis
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Cancer
|
|
4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers .
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-
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- HY-101820A
-
|
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EGFR
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Cancer
|
|
Simotinib hydrochloride is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities .
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-
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- HY-19730A
-
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HM61713 hydrochloride; BI 1482694 hydrochloride
|
EGFR
|
Cancer
|
|
Olmutinib hydrochloride is an orally active and irreversible third EGFR tyrosine kinase inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib hydrochloride is used for NSCLC .
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-
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- HY-100636
-
|
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EGFR
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Cancer
|
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Gefitinib N-oxide is the N-oxide derivative of Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells .
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- HY-144445
-
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EGFR
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Cancer
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NSC114126 is a potent and orally active inhibitor of EGFR tyrosine kinase (EGFR-TK). NSC114126 has strong antiproliferative activities. NSC114126 has the potential for the research of cancer diseases .
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- HY-128893
-
|
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Drug-Linker Conjugates for ADC
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Cancer
|
|
MC-Sq-Cit-PAB-Gefitinib is a agent-linker conjugate for ADC with potent antitumor activity by using Gefitinib (an EGFR tyrosine kinase inhibitor), linked via the ADC linker MC-Sq-Cit-PAB.
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- HY-50895S
-
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ZD1839-d8
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EGFR
Autophagy
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Cancer
|
|
Gefitinib-d8 (ZD1839-d8) is a deuterium labeled Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells .
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- HY-103439
-
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Tyrosine Hydroxylase
EGFR
|
Cancer
|
|
GW 583340 dihydrochloride is an orally active ErbB-2/EGFR tyrosine kinase inhibitor. GW 583340 dihydrochloride exhibits antitumor activity in xenograft models with EGFR overexpression or ErbB-2 overexpression. GW 583340 dihydrochloride is applicable to research related to head and neck cancer, breast cancer, and gastric cancer .
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-
- HY-50895S1
-
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ZD1839-d6
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EGFR
Autophagy
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Cancer
|
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Gefitinib-d6 is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity .
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-
- HY-130616
-
|
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EGFR
Apoptosis
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Cancer
|
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EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFR L858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1 .
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- HY-156741
-
|
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EGFR
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Cancer
|
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EGFR-IN-87 (Compound Example 2) is a EGFR tyrosine kinase inhibitor. EGFR-IN-87 has IC50 value of 3.1 nM, 1.3 nM and 7.1 nM for EGFR_d746-750, EGFR_L858R/T790 and EGFR_WT in A431 cells, respectively. EGFR-IN-87 can be used for cancer diseases research .
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-
- HY-50895AR
-
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ZD-1839 hydrochloride (Standard)
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EGFR
Reference Standards
|
Cancer
|
|
Gefitinib (hydrochloride) (Standard) is the analytical standard of Gefitinib (hydrochloride). This product is intended for research and analytical applications. Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib hydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib hydrochloride also induces autophagy. Gefitinib hydrochloride has antitumour activity .
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-
- HY-110328
-
|
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EGFR
|
Cancer
|
|
PKI-166 hydrochloride is a potent, selective and orally active EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM .
|
-
- HY-112405
-
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PD 159121
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EGFR
|
Cancer
|
|
BPIQ-I (PD 159121) is a potent and ATP-competitive EGFR tyrosine kinase inhibitor.. BPIQ-I shows anti-proliferative actively .
|
-
- HY-50896S1
-
|
CP-358774-13C6; NSC 718781-13C6; OSI-774-13C6
|
Isotope-Labeled Compounds
EGFR
Autophagy
|
Cancer
|
|
Erlotinib- 13C6 is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR .
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-
- HY-100636A
-
|
|
EGFR
|
Cancer
|
|
Gefitinib N-oxide hydrochloride is the N-oxide derivative of Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells .
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-
- HY-19909A
-
|
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EGFR
|
Cancer
|
|
NRC-2694-A is an orally effective EGFR tyrosine kinase inhibitor. NRC-2694-A can be used in the study of malignant squamous cell carcinoma (HNSCC) .
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-
- HY-144444
-
|
|
EGFR
|
Cancer
|
|
NSC381467 is a potent and orally active inhibitor of EGFR tyrosine kinase (EGFR-TK). NSC381467 has strong antiproliferative activities. NSC381467 has the potential for the research of cancer diseases .
|
-
- HY-101820R
-
|
|
Reference Standards
EGFR
|
Cancer
|
|
Simotinib (Standard) is the analytical standard of Simotinib. This product is intended for research and analytical applications. Simotinib is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities .
|
-
- HY-163377
-
|
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Enterovirus
EGFR
|
Infection
|
|
AZ5385 is an EGFR-tyrosine kinase inhibitor. AZ5385 is a HRV-2 virus blocker, with EC50 of 0.35 µM. AZ5385 affects the late stage of viral life cycle .
|
-
- HY-50898C
-
|
GW572016 tosylate; GW2016 tosylate
|
EGFR
Ferroptosis
Autophagy
|
Cancer
|
|
Lapatinib (GW572016) tosylate is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
|
-
- HY-15661A
-
|
CP 373413
|
Drug Metabolite
|
Cancer
|
|
OSI-413 (free base) (CP 373413) is a major metabolite of Erlotinib (HY-50896). Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR .
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-
- HY-118175
-
|
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EGFR
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Others
|
|
RG 14921 is a compound structurally related to Erbstatin (HY-113549) and has inhibitory activity against EGFR tyrosine kinase and CAMP-dependent kinase activity. RG 14921 inhibits EGF receptor kinase activity as a noncompetitive inhibitor.
|
-
- HY-169948
-
|
|
EGFR
|
Cancer
|
|
BML-265 is a potent EGFR tyrosine kinase inhibitor. BML-265 disrupts Golgi integrity and abolishes secretory protein transport of diverse cargos. BML-265 affects Golgi integrity and transport in human cells but not in rodent cells .
|
-
- HY-50898S2
-
|
GW572016-d5; GW2016-d5
|
Isotope-Labeled Compounds
EGFR
Autophagy
Ferroptosis
|
Cancer
|
|
Lapatinib-d5 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
|
-
- HY-50898S3
-
|
GW572016-d4-1; GW2016-d4-1
|
Isotope-Labeled Compounds
EGFR
Autophagy
Ferroptosis
|
Cancer
|
|
Lapatinib-d4-1 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
|
-
- HY-50898R
-
|
GW572016 (Standard); GW2016 (Standard)
|
Reference Standards
EGFR
Autophagy
Ferroptosis
|
Cancer
|
|
Lapatinib (Standard) is the analytical standard of Lapatinib. This product is intended for research and analytical applications. Lapatinib (GW572016) is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
|
-
- HY-145844
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-44 (Compound 6a) is a potent, orally active EGFR tyrosine kinase inhibitor with an IC50 of 4.11 nM. EGFR-IN-44 induces cell apoptosis and shows an oral bioavailability value of 33.57%. EGFR-IN-44 can be studied for non-small-cell lung cancers .
|
-
- HY-13524R
-
-
- HY-18963R
-
|
RG-14355 (Standard)
|
Reference Standards
EGFR
|
Cancer
|
|
Lavendustin A (Standard) is the analytical standard of Lavendustin A. This product is intended for research and analytical applications. Lavendustin A (RG-14355) is a potent, selective and ATP-competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, with an IC50 of 11 nM. Lavendustin A does not inhibit protein kinase A or C. Lavendustin A can suppress VEGF-induced angiogenesis[1][2].
|
-
- HY-50898CS
-
|
GW572016-d4 tosylate; GW2016-d4 tosylate
|
Isotope-Labeled Compounds
EGFR
Autophagy
Ferroptosis
|
Cancer
|
|
Lapatinib-d4 (GW572016-d4) tosylate is deuterium labeled Lapatinib (tosylate). Lapatinib (GW572016) tosylate is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
|
-
- HY-50898BR
-
|
GW572016 ditosylate monohydrate (Standard); GW2016 ditosylate monohydrate (Standard)
|
EGFR
Autophagy
Ferroptosis
Reference Standards
|
Cancer
|
|
Lapatinib (ditosylate monohydrate) (Standard) is the analytical standard of Lapatinib (ditosylate monohydrate). This product is intended for research and analytical applications. Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
|
-
- HY-50898AR
-
|
GW572016 ditosylate (Standard); GW2016 ditosylate (Standard)
|
EGFR
Autophagy
Ferroptosis
Reference Standards
|
Cancer
|
|
Lapatinib (ditosylate) (Standard) is the analytical standard of Lapatinib (ditosylate). This product is intended for research and analytical applications. Lapatinib ditosylate (GW572016 ditosylate) is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
|
-
- HY-131257
-
|
|
Drug Metabolite
|
Others
Cancer
|
|
Gefitinib impurity 1 is the impurity of Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity .
|
-
- HY-W777297
-
|
|
Isotope-Labeled Compounds
EGFR
Autophagy
Ferroptosis
|
Cancer
|
|
Lapatinib- 13C2, 15N Ditosylate is the 13C- and 15N-labeled Lapatinib ditosylate (HY-50898A). Lapatinib ditosylate (GW572016 ditosylate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
|
-
- HY-101958R
-
|
AG82 (Standard); Tyrphostin A 25 (Standard); Tyrphostin AG 82 (Standard); RG-50875 (Standard)
|
Reference Standards
EGFR
GPR35
|
Inflammation/Immunology
Cancer
|
|
Tyrphostin 25 (Standard) (AG82 (Standard)) is the analytical standard of Tyrphostin 25 (HY-101958). This product is intended for research and analytical applications. Tyrphostin 25 (AG82) is a specific inhibitor of the EGFR tyrosine kinase with an IC50 value of 3 µM in A431 cells. Tyrphostin 25 is also a GPR35 agonist with an EC50 of 5.3 µM .
|
-
- HY-100663
-
|
|
EGFR
|
Others
Cancer
|
|
Gefitinib impurity 2 is the impurity of Gefitinib. Gefitinib (ZD1839; HY-50895) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity .
|
-
- HY-50895B
-
|
ZD 1839 dihydrochloride
|
EGFR
Autophagy
Apoptosis
|
Cancer
|
|
Gefitinib (ZD 1839) dihydrochloride is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib dihydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib dihydrochloride also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .
|
-
- HY-133779R
-
|
|
Drug Metabolite
Reference Standards
|
Others
Cancer
|
|
Gefitinib impurity 5 (Standard) is the analytical standard of Gefitinib impurity 5. This product is intended for research and analytical applications. Gefitinib impurity 5 is the impurity of Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity .
|
-
- HY-10322R
-
|
BIBX 1382 (Standard)
|
Reference Standards
EGFR
|
Cancer
|
|
Falnidamol (Standard) is the analytical standard of Falnidamol. This product is intended for research and analytical applications. Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity .
|
-
- HY-163726
-
|
|
GLUT
EGFR
Apoptosis
|
Cancer
|
|
GLUT1/EGFR-IN-1 (compound H) is a potent inhibitor of GLUT1 and EGFR. GLUT1/EGFR-IN-1 can simultaneously act on the EGFR tyrosine kinase ATP-binding site and inhibit GLUT1-mediated energy metabolism, resulting in reductions in ATP, MMP, intra-cellular lactic acid, and EGFR nuclear transfer. GLUT1/EGFR-IN-1 can be used for nasopharyngeal carcinoma (NPC) and triple-negative breast cancer (TNBC) research .
|
-
- HY-50896S3
-
|
CP-358774-d8; NSC 718781-d8; OSI-774-d8
|
Isotope-Labeled Compounds
|
Cancer
|
|
Erlotinib-d8 (CP-358774-d8) is deuterium labeled Erlotinib. Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer . Erlotinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-50896S2
-
|
CP-358774-d4; NSC 718781-d4; OSI-774-d4
|
Isotope-Labeled Compounds
Autophagy
EGFR
|
Cancer
|
|
Erlotinib-d4 (CP-358774-d4) is deuterium labeled Erlotinib. Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer . Erlotinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-12965B
-
|
|
TAM Receptor
|
Cancer
|
|
(Z)-S49076 hydrochloride is an orally active inhibitor of MET and AXL that blocks the downstream signaling of these receptors both in vitro and in vivo, inhibiting the proliferation and migration of tumor cells and suppressing tumor growth in xenograft models. (Z)-S49076 hydrochloride is capable of overcoming the resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) due to MET amplification in Erlotinib (HY-50896)-resistant cell lines both in vitro and in vivo. (Z)-S49076 hydrochloride can be used for research in non-small cell lung cancer (NSCLC) .
|
-
- HY-129510R
-
|
|
EGFR
Mitosis
Reference Standards
|
Cancer
|
|
4-Methyl erlotinib (Standard) is the analytical standard of 4-Methyl erlotinib. This product is intended for research and analytical applications. 4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers .
|
-
- HY-112823R
-
|
HS-10296 (Standard)
|
Reference Standards
EGFR
|
Cancer
|
|
Almonertinib (Standard) is the analytical standard of Almonertinib. This product is intended for research and analytical applications. Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
|
-
- HY-108484R
-
|
|
Reference Standards
EGFR
|
Cancer
|
|
PP 3 (Standard) is the analytical standard of PP 3 (HY-108484). This product is intended for research and analytical applications. PP 3 (Compound 3) is an EGFR tyrosine Kinase inhibitor with an IC50 of 2.7 μM .
|
-
- HY-103439A
-
|
|
Tyrosine Hydroxylase
EGFR
|
Cancer
|
|
GW583340 is an orally active ErbB-2/EGFR tyrosine kinase inhibitor. GW583340 exhibits antitumor activity in xenograft models with EGFR overexpression or ErbB-2 overexpression. GW583340 is applicable to research related to head and neck cancer, breast cancer, and gastric cancer .
|
-
- HY-109189A
-
|
BPI-7711 hydrochloride
|
EGFR
|
Cancer
|
|
Rezivertinib (BPI-7711) hydrochloride is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib hydrochloride exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib hydrochloride has excellent central nervous system (CNS) penetration and has antitumor activity, such as non-small cell lung cancer (NSCLC) .
|
-
- HY-50898S5
-
-
- HY-181166
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-194 is a potent EGFR tyrosine kinase inhibitor with an IC50 of 54.3 nM against human EGFR. EGFR-IN-194 induces apoptosis, inhibits migration in cancer cells, selectively promotes invasion in cancer cells, and exhibits antiproliferative effects across multiple cancer cell lines. EGFR-IN-194 can be used for the research of prostate adenocarcinoma, non-small cell lung carcinoma, breast carcinoma, chronic myeloid leukemia .
|
-
- HY-109061R
-
|
YH25448 (Standard); GNS-1480 (Standard)
|
Apoptosis
Akt
TRP Channel
EGFR
ERK
Reference Standards
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Lazertinib (Standard) is the analytical standard of Lazertinib (HY-109061). This product is intended for research and analytical applications. Lazertinib (YH25448) is a potent, selective, CNS-penetrant, orally available and irreversible EGFR tyrosine Kinase inhibitor, exhibiting high selectivity for activating (EGFRm) and T790M resistance mutations. Lazertinib inhibits phosphorylation of EGFR, AKT and ERK, leading to apoptosis and suppression of tumor growth in mouse H1975-luc brain metastasis xenograft models. Lazertinib can be used in the study of non-small cell lung cancer .
|
-
- HY-173118
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-152 (compound D4) is a potent EGFR tyrosine kinase inhibitor, exhibiting potent EGFR L858R/T790M/C797S inhibition activity (IC50 = 40 nM). EGFR-IN-152 induces G0/G1 phase cell cycle arrest and apoptosis, thereby inhibiting colony formation and cell proliferation of non-small cell lung cancer (NSCLC) cells. EGFR-IN-152 can be used for NSCLC research .
|
-
- HY-109061BR
-
|
YH25448 mesylate (Standard); GNS-1480 mesylate (Standard)
|
Reference Standards
|
Cancer
|
|
Lazertinib mesylate (Standard) is the analytical standard of Lazertinib (mesylate) (HY-109061B). This product is intended for research and analytical applications. Lazertinib (YH25448) mesylate is a potent, selective, CNS-penetrant, orally available and irreversible EGFR tyrosine Kinase inhibitor, exhibiting high selectivity for activating (EGFRm) and T790M resistance mutations. Lazertinib mesylate inhibits phosphorylation of EGFR, AKT and ERK, leading to apoptosis and suppression of tumor growth in mouse H1975-luc brain metastasis xenograft models. Lazertinib mesylate can be used in the study of non-small cell lung cancer .
|
-
- HY-179529
-
|
|
EGFR
Bacterial
|
Infection
Cancer
|
|
EGFR/InhA-IN-1 (Compound 15) is an inhibitor of the anti-cancer target EGFR tyrosine kinase (1M17) (Ki = 0.05 μM) and the anti-tuberculosis target InhA enzyme (1OUZ) (Ki = 0.02 μM). EGFR/InhA-IN-1 exhibits anti-proliferative activity against A549 cells, with an IC50 of 10.38 μM. EGFR/InhA-IN-1 has inhibitory activity against Mycobacterium tuberculosis H37Rv, with a MIC of 6.25 μM. EGFR/InhA-IN-1 can be used for research on non-small cell lung cancer and Mycobacterium tuberculosis infection .
|
-
- HY-P990947
-
|
AZD9592 Antibody
|
ADC Antibody
EGFR
|
Cancer
|
|
Tilatamig (AZD9592 Antibody) is a human antibody of the Ig (G1-κ_G1-λ2) subtype that targets EGFR/MET. Tilatamig conjugates with the Top1 inhibitor AZ14170133 (HY-145399) to form the antibody-drug conjugate (ADC) Tilatamig samrotecan (HY-171124) (AZD9592). Tilatamig accurately targets NSCLC models including EGFR-mutant, EGFR-wildtype, and EGFR tyrosine kinase inhibitor-treated ones, and its activity correlates with high expression of EGFR, c-MET and SLFN11. Tilatamig is available for in vivo anti-tumor studies in patient-derived xenograft models of non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) .
|
-
- HY-112823S
-
|
HS-10296-d6
|
Isotope-Labeled Compounds
EGFR
|
Cancer
|
|
Almonertinib-d6 (HS-10296-d6) is the deuterium labeled Almonertinib (HY-112823). Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
|
-
- HY-131088A
-
|
|
Drug-Linker Conjugates for ADC
EGFR
|
Cancer
|
|
N3-PEG8-Phe-Lys-PABC-Gefitinib TFA is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-tumor agent, Gefitinib (HY-50895) (orally active EGFR tyrosine kinase inhibitor), linked via the cleavable linker N3-PEG8-Phe-Lys-PABC. N3-PEG8-Phe-Lys-PABC-Gefitinib TFA is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-147183
-
|
|
EGFR
|
Cancer
|
|
JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer .
|
-
- HY-147183A
-
|
|
EGFR
|
Cancer
|
|
JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 TFA effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 TFA is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 TFA can be used for researching EGFR-mutant lung cancer .
|
-
- HY-147183B
-
|
|
EGFR
|
Cancer
|
|
JBJ-09-063 hydrochloride is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 hydrochloride effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 hydrochloride is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 hydrochloride can be used for researching EGFR-mutant lung cancer .
|
-
- HY-175864
-
|
|
EGFR
Apoptosis
p38 MAPK
ERK
Akt
STAT
|
Inflammation/Immunology
Cancer
|
|
EGFR-IN-173 is an orally active, pan-mutant EGFR tyrosine kinase inhibitor that targets EGFR 19del, L858R/T790M and C797S triple-mutations, potently inhibiting EGFR 19del/T790M/C797S with an IC50 of 1.19 nM while showing over 100-fold selectivity for mutant over wild-type EGFR (IC50 = 19.362 μM against WT). EGFR-IN-173 significantly inhibits cell migration, induces apoptosis in non-small cell lung cancer (NSCLC) cells. EGFR-IN-173 inhibits EGFR phosphorylation and suppresses the downstream pathways (MAPK/ERK, AKT, STAT3). EGFR-IN-173 exhibits antitumor efficacy in NSCLC and Ba/F3 xenograft models. EGFR-IN-173 can be used for NSCLC research .
|
-
- HY-164392
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
TAS-121 is an orally active, selective, covalent, third-generation mutant EGFR-tyrosine kinase inhibitor (EGFR-TKI). TAS-121 inhibits the L858R mutation (IC50=1.7 nM), Ex19del mutation (IC50=2.7 nM), L858R/T790M mutation (IC50=0.56 nM) and Ex19del/T790M mutation (IC50=1.1 nM) and wild-type EGFR (IC50=8.2 nM). TAS-121 inhibits HER2 and HER4 with IC50s of 110 and 2.6 nM, respectively. TAS-121 inhibits phosphorylation of EGFR and its downstream signaling targets to block cell proliferation. TAS-121 induces apoptosis and displays antitumor activity in SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M) xenograft models .
|
-
- HY-109061A
-
|
YH25448 mesylate hydrate; GNS-1480 mesylate hydrate
|
Apoptosis
Akt
TRP Channel
EGFR
ERK
|
Cancer
|
|
Lazertinib (YH25448; GNS-1480) mesylate hydrate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate hydrate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate hydrate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate hydrate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate hydrate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
|
-
- HY-109061B
-
|
YH25448 mesylate; GNS-1480 mesylate
|
TRP Channel
EGFR
Akt
ERK
Apoptosis
|
Cancer
|
|
Lazertinib (YH25448; GNS-1480) mesylate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
|
-
- HY-109061
-
|
YH25448; GNS-1480
|
Apoptosis
Akt
TRP Channel
EGFR
ERK
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Lazertinib (YH25448; GNS-1480) is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
|
-
| Art. -Nr. |
Produktname |
Type |
-
- HY-50895G
-
|
ZD1839
|
Fluorescent Dyes
|
|
Gefitinib (ZD1839) (GMP) is Gefitinib (HY-50895) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Gefitinib is a potent, selective and orally active EGFR tyrosine kinase inhibitor .
|
| Art. -Nr. |
Produktname |
Type |
-
- HY-50895G
-
|
ZD1839
|
Biochemical Assay Reagents
|
|
Gefitinib (ZD1839) (GMP) is Gefitinib (HY-50895) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Gefitinib is a potent, selective and orally active EGFR tyrosine kinase inhibitor .
|
| Art. -Nr. |
Produktname |
Target |
Research Area |
Image |
-
- HY-P990947
-
|
AZD9592 Antibody
|
ADC Antibody
EGFR
|
Cancer
|
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Tilatamig (AZD9592 Antibody) is a human antibody of the Ig (G1-κ_G1-λ2) subtype that targets EGFR/MET. Tilatamig conjugates with the Top1 inhibitor AZ14170133 (HY-145399) to form the antibody-drug conjugate (ADC) Tilatamig samrotecan (HY-171124) (AZD9592). Tilatamig accurately targets NSCLC models including EGFR-mutant, EGFR-wildtype, and EGFR tyrosine kinase inhibitor-treated ones, and its activity correlates with high expression of EGFR, c-MET and SLFN11. Tilatamig is available for in vivo anti-tumor studies in patient-derived xenograft models of non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) .
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(5)
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Produktname |
Category |
Target |
Chemical Structure |
| Art. -Nr. |
Produktname |
Chemical Structure |
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- HY-50898S4
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Lapatinib-d7 (GW572016-d7) is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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- HY-50896S
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Erlotinib-d6 (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR . Erlotinib-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-15772S3
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Asandeutertinib (Osimertinib-d3; AZD-9291-d3) is a epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, with antineoplastic effect .
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- HY-50895S2
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Gefitinib-d3 (ZD1839-d3) is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity .
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- HY-50898S1
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Lapatinib-d7 dihydrochloride is the deuterium labeled Lapatinib dihydrochloride. Lapatinib (GW572016) dihydrochloride is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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- HY-50898S
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Lapatinib-d4 is the deuterium labeled Lapatinib (HY-50898). Lapatinib is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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- HY-50895S
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Gefitinib-d8 (ZD1839-d8) is a deuterium labeled Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells .
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- HY-50895S1
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Gefitinib-d6 is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity .
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- HY-50896S1
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Erlotinib- 13C6 is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR .
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- HY-50898S2
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Lapatinib-d5 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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- HY-50898S3
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Lapatinib-d4-1 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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- HY-50898CS
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Lapatinib-d4 (GW572016-d4) tosylate is deuterium labeled Lapatinib (tosylate). Lapatinib (GW572016) tosylate is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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- HY-W777297
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Lapatinib- 13C2, 15N Ditosylate is the 13C- and 15N-labeled Lapatinib ditosylate (HY-50898A). Lapatinib ditosylate (GW572016 ditosylate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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- HY-50896S3
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Erlotinib-d8 (CP-358774-d8) is deuterium labeled Erlotinib. Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer . Erlotinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-50896S2
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Erlotinib-d4 (CP-358774-d4) is deuterium labeled Erlotinib. Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer . Erlotinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-50898S5
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Lapatinib- 13C,d7 (GW572016- 13C,d7) is the deuterium and 13C-labeled Lapatinib (HY-50898). Lapatinib (GW572016) is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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- HY-112823S
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Almonertinib-d6 (HS-10296-d6) is the deuterium labeled Almonertinib (HY-112823). Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
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| Art. -Nr. |
Produktname |
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Classification |
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- HY-50896
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CP-358774; NSC 718781; OSI-774
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Alkynes
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Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer . Erlotinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-139300
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HMPL-813
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Alkynes
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Epitinib (HMPL-813) is a selective, orally active, blood-brain barrier-permeable EGFR tyrosine kinase inhibitor. Epitinib is applicable to research on EGFR T790M-positive non-small cell lung cancer with brain metastasis and advanced solid tumors .
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- HY-131088
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ADC Synthesis
Azide
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N3-PEG8-Phe-Lys-PABC-Gefitinib is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-tumor agent, Gefitinib (HY-50895) (orally active EGFR tyrosine kinase inhibitor), linked via the cleavable linker N3-PEG8-Phe-Lys-PABC. N3-PEG8-Phe-Lys-PABC-Gefitinib is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-50896S
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CP-358774-d6; NSC 718781-d6; OSI-774-d6
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Alkynes
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Erlotinib-d6 (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR . Erlotinib-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-129510
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Alkynes
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4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers .
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- HY-131088A
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Azide
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N3-PEG8-Phe-Lys-PABC-Gefitinib TFA is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-tumor agent, Gefitinib (HY-50895) (orally active EGFR tyrosine kinase inhibitor), linked via the cleavable linker N3-PEG8-Phe-Lys-PABC. N3-PEG8-Phe-Lys-PABC-Gefitinib TFA is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-50896S1
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CP-358774-13C6; NSC 718781-13C6; OSI-774-13C6
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Alkynes
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Erlotinib- 13C6 is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR .
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- HY-15661A
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CP 373413
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Alkynes
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OSI-413 (free base) (CP 373413) is a major metabolite of Erlotinib (HY-50896). Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR .
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| Art. -Nr. |
Produktname |
Target |
Forschungsgebiete |
Chemical Structure |
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- HY-50895G
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ZD1839
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EGFR
Autophagy
Apoptosis
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Cancer
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Gefitinib (ZD1839) (GMP) is Gefitinib (HY-50895) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Gefitinib is a potent, selective and orally active EGFR tyrosine kinase inhibitor .
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