AST-1306|cas 1050500-29-2|DC Chemicals|Price|Buy

Cas No.:	1050500-29-2
Chemical Name:	N-[4-[[3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl]amino]quinazolin-6-yl]acrylamide tosylate
Synonyms:	Allitinib tosylate; AST1306 TsOH; AST-1306 TsOH; AST 1306 TsOH; ALS1306 TsOH; ALS-1306 TsOH; ALS1306 TsOH; AST 6 TsOH; AST-6 TsOH; AST6 TsOH.
SMILES:	FC1=CC=CC(COC2=C(Cl)C=C(NC3=NC=NC4=C3C=C(NC(C=C)=O)C=C4)C=C2)=C1.O=S(C5=CC=C(C)C=C5)(O)=O
Formula:	C₃₁H₂₆ClFN₄O₅S
M.Wt:	621.0804
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

AST-1306 also ErB2 and EGFR T790M/L858R double mutant. AST-1306 is approximately 500-fold more potent than lapatinib and more than 3000-fold selective For ErbB family kinases over other kinase families including PDGFR, KDR and c-Met. AST-1306 might covalently bind to specific amino acid residues of EGFR and ErbB2. AST-1306 acts in a concentration dependent manner to significantly inhibit the growth of HIH3T3-EGFR T790M/L858R cells. AST-1306 effectively suppresses EGFR phosphorylation in HIH3T3-EGFR T790M/L858R cells. Moreover, AST-1306 blocks the growth of NCI-H1975 cells that harbor the EGFR T790M/L858R mutation in a concentration-dependent manner. AST-1306 blocks phosphorylation of EGFR and downstream pathways as well. In addition, AST-1306 dose-dependently and markedly inhibits EGF-induced EGFR phosphorylation in A549 cells. AST-1306 inhibits the phosphorylation of EGFR and ErbB2, and downstream signaling in human cancer cells including A549 cells, Calu-3 cells and SK-OV-3 cells. Twice daily oral administration of AST-1306 gives rise to a dramatic prevention of tumor growth in SK-OV-3 and Calu-3 xenograft models. In SK-OV-3 models, tumors nearly disappears after treatment with AST-1306 For 7 days. In contrast, AST-1306 only slightly inhibits the growth of tumor in HO-8910 and A549 xenograft models. There Fore, the antitumor efficacy of AST-1306 is greater in ErbB2-overexpressing tumor models than in models expressing low levels of ErbB2. AST-1306 is well tolerated. Lapatinib displays antitumor activity in these ErbB2-overexpressing tumor models, but AST-1306 is more efficacious than lapatinib in the SK-OV-3 xenograft tumor model when given at the same dose and schedule. In addition, oral administration of AST-1306 twice daily For 3 weeks dramatically suppresses the growth of tumor in the FVB-2/Nneu models. After treatment For 11 days, tumors almost completely disappears. The body weights of the mice reduces by less than 20% during treatment. For the detailed information of AST-1306, the solubility of AST-1306 in water, the solubility of AST-1306 in DMSO, the solubility of AST-1306 in PBS buffer, the animal experiment (test) of AST-1306, the cell expriment (test) of AST-1306, the in vivo, in vitro and clinical trial test of AST-1306, the EC50, IC50,and Affinity of AST-1306, Please contact DC Chemicals.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC8253	AV-412(MP-412)	AV-412(MP-412) is a potent dual inhibitor of EGFR and ErbB2(IC50=19 nM) tyrosine kinases, including the mutant EGFR(L858R IC50=0.51 nM, T790M IC50=0.79 nM); inhibits autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively.
DC7360	AST-1306	AST-1306 is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases.