AST-1306 is a novel irreversible epidermal growth factor receptor inhibitor for EGFR and ErbB4 with IC50 of 0.5 and 0.8 nM, respectively. AST-1306 selectively inhibits the tyrosine kinase activities of ErbB2 with an IC50 of 3 nM. AST-1306 also potently prevents the EGFR T790M/L858R double mutant with an IC50 value of 12 nM.

By VD/VDR- vd-vdr June 21, 2017

prudect name : AST-1306 is a novel irreversible epidermal growth factor receptor inhibitor for EGFR and ErbB4 with IC50 of 0.5 and 0.8 nM, respectively. AST-1306 selectively inhibits the tyrosine kinase activities of ErbB2 with an IC50 of 3 nM. AST-1306 also potently prevents the EGFR T790M/L858R double mutant with an IC50 value of 12 nM.
AST-1306

Synonyms: CAS NO: 1050500-29-2Molecular Formula: C₂₄H₁₈ClFN₄O₂,C₇H₈O₃SMolecular Weight: 621.08Purity: 98% minSolubility: In DMSOStorage: −20°C

128517-07-7 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18500230

AST1306 is a novel anilino-quinazoline compound, which inhibits the enzymatic activities of wild-type epidermal growth factor receptor (EGFR) and ErbB2 as well as EGFR resistant mutant in both cell-free and cell-based systems. AST1306 was found to function as an irreversible inhibitor, most likely through covalent interaction with Cys797 and Cys805 in the catalytic domains of EGFR and ErbB2, respectively. In vivo, AST1306 potently suppressed tumor growth in ErbB2-overexpressing adenocarcinoma xenograft and FVB-2/N(neu) transgenic breast cancer mouse models, but weakly inhibited the growth of EGFR-overexpressing tumor xenografts. Tumor growth inhibition induced by a single dose of AST1306 in the SK-OV-3 xenograft model was accompanied by a rapid (within 2 h) and sustained (≥24 h) inhibition of both EGFR and ErbB2, consistent with an irreversible inhibition mechanism. Taken together, these results establish AST1306 as a selective, irreversible ErbB2 and EGFR inhibitor whose growth-inhibitory effects are more potent in ErbB2-overexpressing cells.

By VD/VDR- vd-vdr June 21, 2017

prudect name : AST1306 is a novel anilino-quinazoline compound, which inhibits the enzymatic activities of wild-type epidermal growth factor receptor (EGFR) and ErbB2 as well as EGFR resistant mutant in both cell-free and cell-based systems. AST1306 was found to function as an irreversible inhibitor, most likely through covalent interaction with Cys797 and Cys805 in the catalytic domains of EGFR and ErbB2, respectively. In vivo, AST1306 potently suppressed tumor growth in ErbB2-overexpressing adenocarcinoma xenograft and FVB-2/N(neu) transgenic breast cancer mouse models, but weakly inhibited the growth of EGFR-overexpressing tumor xenografts. Tumor growth inhibition induced by a single dose of AST1306 in the SK-OV-3 xenograft model was accompanied by a rapid (within 2 h) and sustained (≥24 h) inhibition of both EGFR and ErbB2, consistent with an irreversible inhibition mechanism. Taken together, these results establish AST1306 as a selective, irreversible ErbB2 and EGFR inhibitor whose growth-inhibitory effects are more potent in ErbB2-overexpressing cells.
AST-1306

Synonyms: CAS NO: 897383-62-9Molecular Formula: C₂₄H₁₈ClFN₄O₂Molecular Weight: 448.88Purity: 98% minSolubility: In DMSOStorage: -20°C

2353-33-5 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18502633

By VD/VDR- vd-vdr

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