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Submit ReviewAZD 9291 is a potent mutant-selective EGFR inhibitor (IC50 values are 1 and 12 nM against EGFR mutants L858R/T790M and L858R, respectively). AZD 9291 exhibited nearly 200 times greater potency against L858R/T790M than wild-type EGFR. In vivo, AZD 9291 causes tumor regression in mutant EGFR xenograft models of non-small cell lung cancer (NSCLC) and transgenic mutant T790M EGFR disease models. AZD 9291 is orally bioavailable.
分子量 | 499.61 |
公式 | C28H33N7O2 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1421373-65-0 |
PubChem ID | 71496458 |
InChI Key | DUYJMQONPNNFPI-UHFFFAOYSA-N |
Smiles | O=C(C=C)NC1=CC(NC=2N=CC=C(N2)C3=CN(C=4C=CC=CC34)C)=C(OC)C=C1N(C)CCN(C)C |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 24.98 | 50 | |
ethanol | 9.99 | 20 |
以下数据基于产品分子量 499.61。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 4 mL | 20.02 mL | 40.03 mL |
2.5 mM | 0.8 mL | 4 mL | 8.01 mL |
5 mM | 0.4 mL | 2 mL | 4 mL |
25 mM | 0.08 mL | 0.4 mL | 0.8 mL |
参考文献是支持产品生物活性的出版物。
Cross et al (2014) AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 4 1046 PMID: 24893891
If you know of a relevant reference for AZD 9291, please let us know.
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