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Sapitinib

Chemical Structure : Sapitinib

CAS No.: 848942-61-0

Sapitinib (AZD-8931, AZD8931)

货号: PC-43354Not For Human Use, Lab Use Only.

Sapitinib (AZD-8931, AZD8931) is a equipotent, reversible inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4. 3 and 4 nM (phosphorylation inhibition), respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Sapitinib (AZD-8931, AZD8931) is a equipotent, reversible inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4. 3 and 4 nM (phosphorylation inhibition), respectively.
Sapitinib (AZD-8931) displays >1,000-fold selectivity over a panel of 206 of kinases, >100-fold selectivity for MNK1 and Flt3.
Sapitinib (AZD-8931) is significantly more potent than gefitinib or lapatinib in specific squamous cell carcinoma of the head and neck and non-small cell lung carcinoma cell lines.
Sapitinib (AZD-8931) inhibits xenograft growth in a range of models while significantly affecting EGFR, erbB2, and erbB3 phosphorylation and downstream signaling pathways, apoptosis, and proliferation.

物理化学性质&存储条件

分子量 473.9277
分子式 C23H25ClFN5O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 33 mg/mL

Chemical Name/SMILES

1-Piperidineacetamide, 4-[[4-[(3-chloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]oxy]-N-methyl-

参考文献

1. Hickinson DM, et al. Clin Cancer Res. 2010 Feb 15;16(4):1159-69.

2. Singleton KR, et al. Mol Pharmacol. 2013 Apr;83(4):882-93.

3. Barlaam B, et al. ACS Med Chem Lett. 2013 May 31;4(8):742-6.

4. Mu Z, et al. J Exp Clin Cancer Res. 2014 May 30;33:47.

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