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Chemical Structure : Sapitinib
CAS No.: 848942-61-0
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $128 | In stock | |
| 25 mg | $198 | In stock | |
| 50 mg | Get quote | ||
| 100 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.
| M.Wt | 473.9277 | |
| Formula | C23H25ClFN5O3 | |
| Appearance | Solid | |
| Storage |
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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- |
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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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