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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
441 Results for "
her2
" in MedChemExpress (MCE) Product Catalog:
Products (441)
441 Results for "her2" in MCE Product Catalog:
11
11 Cited Publications
Cat. No.: HY-P9912
CAS No.: 380610-27-5
9
9 Cited Publications
Synonyms: HM781-36B; NOV120101
Poziotinib (HM781-36B) is an orally active, irreversible pan-HER inhibitor, which effectively inhibits EGFR wt, HER-2 and HER-4 with IC50s of 3.2, 5.3 and 23.5 nM, respectively. Poziotinib (HM781-36B) also shows excellent inhibitory activities against mutated EGFRs, including EGFR T790M and EGFR L858R/T790M, with IC50s of 4.2 and 2.2 nM, respectively. Excellent antitumor activity [2].
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Mubritinib (TAK-165) is a potent and selective EGFR2/HER2 inhibitor with an IC50 of 6 nM.
8
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Camizestrant (AZD-9833) is a potent and orally active estrogen receptor (ER) antagonist. Camizestrant is used for the study of ER + HER2-advanced breast cancer .
8
8 Cited Publications
Cat. No.: HY-P9921
CAS No.: 1018448-65-1
Synonyms: Ado-Trastuzumab emtansine; PRO132365; T-DM 1
8
8 Cited Publications
Cat. No.: HY-P9921A
CAS No.: 1018448-65-1
Synonyms: Ado-Trastuzumab emtansine (solution) ; PRO132365 (solution) ; T-DM 1 (solution)
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Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1 (derivative of maytansine), and the drug-linker conjugate for ADC is SMCC-DM1 (HY-101070). Trastuzumab emtansine can be used for the research of advanced breast cancer [2].
7
7 Cited Publications
CUDC-101 is a potent inhibitor of HDAC, EGFR, and HER2 with IC50s of 4.4, 2.4, and 15.7 nM, respectively. CUDC-101 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
5
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Disitamab vedotin (RC48) is a HER2-targeted antibody-drug conjugate (ADC), formed by conjugation of the humanized anti-HER2 antibody Disitamab (HY-P99854) with drug-linker VcMMAE (HY-15575). VcMMAE consists of a cleavable MC-Val-Cit-PAB linker and the microtubule inhibitor MMAE (HY-15162). After binding to HER2 and undergoing endocytosis, Disitamab vedotin releases MMAE in lysosomes, which further inhibits microtubule assembly, arrests mitosis and induces apoptosis, while also exerting a bystander effect. Disitamab vedotin can be used in studies of HER2-positive breast cancer [2] .
4
4 Cited Publications
CP-724714 is an orally active and selective HER2 tyrosine kinase inhibitor with an IC50 of 10 nM. CP-724714 inhibits HER2 receptor autophosphorylation and blocks the downstream Ras-Raf-Mek-Erk signaling pathway, thereby inducing cell cycle arrest and apoptosis in tumor cells. CP-724714 exhibits antiviral activity and inhibits various porcine diarrheal coronaviruses, including SADS-CoV (IC50 of 0.91 μM). CP-724714 is an inhibitor of the hepatic transport receptors OATP1B1/MDR1/BSEP, and can enter hepatocytes via active uptake and trigger the accumulation of drugs and bile acids within hepatocytes. CP-724714 can be used in research related to HER2-overexpressing breast cancer and porcine diarrheal coronavirus infection [2] .
4
Sunvozertinib (DZD9008) is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC50s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52) .
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4 Cited Publications
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ZCL278 is a selective Cdc42 inhibitor with Kds of 6.4 μM in fluorescence titration and 11.4 μM in surface plasmon resonance (SPR) measurement. ZCL278 is able to disrupt the Cdc42-ITSN interaction as well as GTP/GDP binding. ZCL278 has inhibitory effects on various enveloped viruses, but is ineffective against non-enveloped viruses. ZCL278 can be used for the studies of arsenic neurotoxicity and HER2-positive gastric cancer (GC) [2] .
4
SNX-2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a Kd of 16 nM for Hsp90 and IC50s of 30 nM, 30 nM for Hsp90 α and Hsp90 β, also induces Her-2 degradation, and inhibits Grp94 and Trap-1, with IC50s of 10 nM, 4.275 μM and 0.862 μM, respectively . SNX-2112 (PF 04928473) binds Hsp90 isoforms Hsp90α, Hsp90β and Hsp90b1/Grp94 with Kds of 4 nM, 6 nM and 484 nM, respectively [2].
4
4 Cited Publications
Synonyms: XL-647; EXEL-7647; KD-019
Tesevatinib (XL-647) is an orally available, blood-brain barrier-penetrant inhibitor of the epidermal growth factor receptor (EGFR). Tesevatinib significantly reduces cellular viability, with IC50 values of 11 nM and 102 nM in GBM12 and GBM6, respectively. Tesevatinib also inhibits HER2 (IC50=16.1 nM), VEGFR2 (IC50=1.5 nM), and Src (IC50=10.3 nM). Tesevatinib can inhibit tumor proliferation and exhibits antitumor activity [2].
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3
3 Cited Publications
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H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer [2].
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3 Cited Publications
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H3B-6545 hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer [2].
3
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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 [2] .
3
BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy [2].
3
3 Cited Publications
Synonyms: AC480 Hydrochloride
BMS-599626 Hydrochloride (AC480 Hydrochloride) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 Hydrochloride displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 Hydrochloride inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy [2].
3
3 Cited Publications
TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity . TAK-285 can cross the blood-brain barrier (BBB) [2].
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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
