A dual inhibitor of EGFR and HER2 (IC50s = 1.4

AV-412 – 25 mg

Brand:
Cayman
CAS:
451493-31-5
Storage:
-20
UN-No:
Non-Hazardous - /

AV-412 is a dual inhibitor of EGFR and HER2 (IC50s = 1.4, 0.51, 0.79, 2.3, and 19 nM for the EGFR, EGFRL858R, EGFRT790M, EGFRL858R,T790M, and HER2 recombinant intracellular kinase domains, respectively).{46529} It is selective for EGFR and HER2 over IRK, MEK1, PKA, and PKC (IC50s = >10 μM) but also inhibits Abl, FLT1, and Src (IC50s = 41, 920, and 2,000 nM, respectively). AV-412 (10 and 30 μM) induces ubiquitination and degradation of HER2 in SK-BR-3 cells.{46530} It decreases levels of HER2 and estrogen receptor α (ERα) and increases levels of Hsp70 in MCF-7 cells when used at a concentration of 10 μM. AV-412 inhibits EGF-stimulated growth of A431 cells (IC50 = 0.1 μM).{46529} It reduces tumor growth in an A431 mouse xenograft model when administered at doses of 10 and 30 mg/kg and in a BT-474 mouse xenograft model at 30 mg/kg.  

 

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SKU: 29039 - 25 mg Category:

Description

A dual inhibitor of EGFR and HER2 (IC50s = 1.4, 0.51, 0.79, 2.3, and 19 nM for the EGFR, EGFRL858R, EGFRT790M, EGFRL858R,T790M, and HER2 recombinant intracellular kinase domains, respectively); selective for EGFR and HER2 over IRK, MEK1, PKA, and PKC (IC50s = >10 μM) but also inhibits Abl, FLT1, and Src (IC50s = 41, 920, and 2,000 nM, respectively); induces ubiquitination and degradation of HER2 in SK-BR-3 cells at 10 and 30 μM; decreases levels of HER2 and ERα and increases levels of Hsp70 in MCF-7 cells at 10 μM; inhibits EGF-stimulated growth of A431 cells (IC50 = 0.1 μM); reduces tumor growth in an A431 mouse xenograft model at 10 and 30 mg/kg and in a BT-474 mouse xenograft model at 30 mg/kg

Formal name: N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-methyl-3-(4-methyl-1-piperazinyl)-1-butyn-1-yl]-6-quinazolinyl]-2-propenamide, 4-methylbenzenesulfonate (1:2)

Synonyms:  MP-412

Molecular weight: 851.4

CAS: 451493-31-5

Purity: ≥98%

Formulation: A solid

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