A dual inhibitor of EGFR and HER2 (IC50s = 22 and 32 nM

AC480 – 1 mg

Brand:
Cayman
CAS:
714971-09-2
Storage:
-20
UN-No:
Non-Hazardous - /

AC480 is a dual inhibitor of EGFR and HER2 (IC50s = 22 and 32 nM, respectively).{52241} It is selective for EGFR and HER2 over HER4 (IC50 = 190 nM) and a panel of 21 additional kinases (IC50s = >2,500 nM for all). AC480 inhibits proliferation in a panel of EGFR and/or HER2 signaling-dependent cancer cells (IC50s = 0.24-0.94 μM). It reduces tumor growth in a Sal2 murine salivary gland tumor model, as well as GEO colon and KPL4 breast cancer mouse xenograft models in a dose-dependent manner. AC480 (100 mg/kg) reduces tumor cell motility, intravasation, and EGF-induced invasion in an MTLn3E metastatic mammary adenocarcinoma mouse xenograft model.{52242}  

 

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SKU: 29657 - 1 mg Category:

Description

A dual inhibitor of EGFR and HER2 (IC50s = 22 and 32 nM, respectively); selective for EGFR and HER2 over HER4 (IC50 = 190 nM) and a panel of 21 additional kinases (IC50s = >2,500 nM for all); inhibits proliferation in a panel of EGFR and/or HER2 signaling-dependent cancer cells (IC50s = 0.24-0.94 μM); reduces tumor growth in a Sal2 murine salivary gland tumor model, as well as GEO colon and KPL4 breast cancer mouse xenograft models in a dose-dependent manner; reduces tumor cell motility, intravasation, and EGF-induced invasion in an MTLn3E metastatic mammary adenocarcinoma mouse xenograft model at 100 mg/kg

Formal name: N-[4-[[1-[(3-fluorophenyl)methyl]-1H-indazol-5-yl]amino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]-carbamic acid, (3S)-3-morpholinylmethyl ester

Synonyms:  BMS-599626

Molecular weight: 530.6

CAS: 714971-09-2

Purity: ≥98%

Formulation: A cystalline solid

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