Chemical Structure : Sapitinib
CAS No.: 848942-61-0
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.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | ¥880 | In stock | |
25 mg | ¥1380 | In stock | |
50 mg | ¥2180 | In stock | |
100 mg | ¥3580 | In stock | |
250 mg | Get quote |
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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.
分子量 | 473.9277 | |
分子式 | C23H25ClFN5O3 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
DMSO: ≥ 33 mg/mL |
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Chemical Name/SMILES |
1-Piperidineacetamide, 4-[[4-[(3-chloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]oxy]-N-methyl- |
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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