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Description: Potent mutant-selective EGFR inhibitor
Chemical Name: N-[2-[[2-(Dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide
Purity: ≥98% (HPLC)
Biological Activity for AZD 9291
AZD 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.
Technical Data for AZD 9291
| M. Wt | 499.61 |
| Formula | C28H33N7O2 |
| Storage | Store at -20°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for AZD 9291
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 24.98 | 50 | |
| ethanol | 9.99 | 20 |
Preparing Stock Solutions for AZD 9291
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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 |
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Product Datasheets for AZD 9291
References for AZD 9291
References are publications that support the biological activity of the product.
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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Citations for AZD 9291
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