An irreversible EGFR

AST-1306 (tosylate) – 10 mg

Brand:
Cayman
CAS:
1050500-29-2
Storage:
-20
UN-No:
Non-Hazardous - /

AST-1306 is an irreversible inhibitor of EGFR, HER2, and HER4 (IC50s = 0.5, 3, and 0.8 nM, respectively).{48897} It is selective for EGFR, HER2, and HER4 over a panel of 23 additional kinases (IC50s = >10 µM). AST-1306 also inhibits EGFRT790M/L858R with an IC50 value of 12 nM in a cell-free assay. It decreases EGFR, ERK1/2, and Akt phosphorylation in Calu-3, A549, and SKOV3 cancer cells when used at concentrations ranging from 0.001 to 1 µM. AST-1306 inhibits proliferation of Calu-3, BT474, MDA-MB-468, A549, SKOV3, NCI H23, and MCF-7 cells (IC50s = 0.23-16 µM). It reduces tumor growth in Calu-3, A549, SKOV3, and HO8910 mouse xenograft models when administered at doses of 25, 50, and 100 mg/kg per day.  

 

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SKU: 29708 - 10 mg Category:

Description

An irreversible EGFR, HER2, and HER4 inhibitor (IC50s = 0.5, 3, and 0.8 nM, respectively); selective for EGFR, HER2, and HER4 over a panel of 23 additional kinases (IC50s = >10 µM); inhibits EGFRT790M/L858R (IC50 = 12 nM in a cell-free assay); decreases EGFR, ERK1/2, and Akt phosphorylation in Calu-3, A549, and SKOV3 cancer cells from 0.001-1 µM; inhibits proliferation of various cancer cells (IC50s = 0.23-16 µM); reduces tumor growth in Calu-3, A549, SKOV3, and HO8910 mouse xenograft models at 25, 50, and 100 mg/kg per day

Formal name: N-[4-[[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-6-quinazolinyl]-2-propenamide, 4-methylbenzenesulfonate

Synonyms:  Allitinib

Molecular weight: 621.1

CAS: 1050500-29-2

Purity: ≥98%

Formulation: A crystalline solid

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