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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
28 Results for "
wild-type EGFR kinase
" in MedChemExpress (MCE) Product Catalog:
Products (28)
28 Results for "wild-type EGFR kinase" in MCE Product Catalog:
10
10 Publications Verification
Synonyms: HS-10296
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 .
10
10 Publications Verification
Synonyms: HS-10296 mesylate
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 .
10
10 Publications Verification
Synonyms: HS-10296 hydrochloride
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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3 Cited Publications
Synonyms: BDTX-1535; EGFR-IN-76
Target:
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Silevertinib (BDTX-1535) is an irreversible, brain-penetrant, selective and orally active EGFR inhibitor with wild-type EGFR-sparing. Silevertinib targets key EGFR resistance mutations, including the kinase domain (C797S, L718Q, G724S, S768I), extracellular domain (EGFRvIII, A289X), and EGFR amplification. Silevertinib exerts anti-tumor activity with well tolerated in vivo. Silevertinib can be used for non-small cell lung cancer (NSCLC) and glioblastoma (GBM) research .
Cat. No.: HY-19815
CAS No.: 1660963-42-7
Synonyms: CK-101; RX518
Olafertinib (CK-101) is an orally available, third generation and irreversible epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI). Olafertinib selectively inhibits both EGFR-TKI-sensitizing and resistance mutations with minimal activity on wild-type EGFR. Olafertinib can be used in research for non-small cell lung cancer (NSCLC) with EGFR mutations and other advanced malignancies .
Synonyms: Brigatinib analog
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ALK-IN-1 is an orally active, blood-brain barrier-permeable ALK and EGFR inhibitor. ALK-IN-1 binds to and inhibits ALK kinase, ALK fusion proteins, and wild-type and mutant EGFR variants, thereby disrupting their corresponding signaling pathways. ALK-IN-1 can suppress the growth and proliferation of tumor cells and exhibits potential inhibitory activity against mutant EGFR. ALK-IN-1 can be used in the research of non-small-cell lung cancer .
Cat. No.: HY-161275
CAS No.: 2769715-68-4
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BI-4732 is an orally active, reversible, ATP-competitive EGFR inhibitor with blood-brain barrier penetration. BI-4732 inhibits the kinase activity of EGFR L858R, T790M and C797S with IC50 values of 1 nM while sparing EGFR wild-type. BI-4732 inhibits EGFR and reduces the phosphorylation of AKT, ERK, and S6K. BI-4732 demonstrates excellent intracranial anti-tumor efficacy in YU-1097 xenograft model harboring EGFR_E19del/T790M/C797S. BI-4732 can be used for the study of non-small cell lung cancer (NSCLC) .
Cat. No.: HY-153974
CAS No.: 2254805-44-0
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BBT-176 is an orally active EGFR tyrosine kinase inhibitor. BBT-176 is a reversible ATP-competitive inhibitor with a unique binding mode, and it exhibits selectivity for mutant EGFR over wild-type EGFR. BBT-176 inhibits tumor growth, induces tumor regression, upregulates EGFR expression, and does not trigger secondary EGFR gene mutations. BBT-176 can be used in research related to non-small cell lung cancer .
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DZD1516 is an orally active, reversible, blood-brain barrier (BBB)-penetrant selective HER2 tyrosine kinase inhibitor with an IC50 of 0.56 nM against HER2. DZD1516 is not a substrate of P-gp or BCRP, and exhibits high passive permeability. DZD1516 inhibits tumor growth in HER2-positive brain metastasis, leptomeningeal metastasis and subcutaneous xenograft models, and can be used for research related to HER2-positive breast cancer and central nervous system metastasis .
Cat. No.: HY-161633
CAS No.: 3034244-71-5
PROTAC EGFR degrader 11 (Compound B71) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC50 <100 nM. PROTAC EGFR degrader 11 binds CRBN-DDB1 with a Ki of 36 nM. PROTAC EGFR degrader 11 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC50 <100 nM.
Cat. No.: HY-P990947
CAS No.: 2868265-50-1
Synonyms: AZD9592 Antibody
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CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ～10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines .
Cat. No.: HY-W740378
CAS No.: 220038-19-7
Synonyms: AFN-941
1,2,3,4-Tetrahydrostaurosporine is a derivative of Staurosporine (HY-15141) and an inhibitor of mutant EGFR (IC50=74 nM for EGFRT790M). It is selective for EGFRT790M over wild-type EGFR (IC50=390 nM). It also binds to Janus kinase 3 (JAK3).
Cat. No.: HY-161632
CAS No.: 3034244-56-6
PROTAC EGFR degrader 10 (Compound B56) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC50 <100 nM. PROTAC EGFR degrader 10 binds CRBN-DDB1 with a Ki of 37 nM. PROTAC EGFR degrader 10 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC50 <150 nM .
Cat. No.: HY-175864
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 .
Cat. No.: HY-164392
CAS No.: 1451370-01-6
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 .
Cat. No.: HY-164056
CAS No.: 333419-97-9
EGFR T790M/L858R-IN-8 (Compound 9) is a selective EGFR T790M/L858R mutant kinase inhibitor with a IC50 of 56.8 μM, and it shows no inhibitory activity against wild-type EGFR. EGFR T790M/L858R-IN-8 can be used for the research of non-small cell lung cancer .
Cat. No.: HY-171252
CAS No.: 852407-49-9
EGFR-IN-145 (compound 7c) is an EGFR kinase inhibitor. At a concentration of 20 μM, EGFR-IN-145 has an inhibition rate of 52.7% on EGFR-wild type kinase .
Cat. No.: HY-149099
CAS No.: 2918281-79-3
RET-IN-22 (compound 17b) is a potent, selective and orally active RET inhibitor with an IC50 of 20.9 nM and 18.3 nM for wild-type RET and RET-V804M, respectively. RET-IN-22 shows highly selective profile to most kinases, especially to EGFR and VEGFR2. RET-IN-22 has anticancer effects .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
