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Sapitinib

Chemical Structure : Sapitinib

CAS No.: 848942-61-0

Sapitinib (AZD-8931, AZD8931)

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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 473.9277
Formula C23H25ClFN5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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-

References

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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