AZD 9291

Name: AZD 9291
Brand: Tocris Bioscience
SKU: 8873

Tocris Bioscience, part of Bio-Techne | Catalog # 8873

COA / SDS

Potent mutant-selective EGFR inhibitor

Key Product Details

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)
Molecular Weight:	499.61

View Full Technical Details for AZD 9291

Technical Data
Citations

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 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	4.00 mL	20.02 mL	40.03 mL
2.5 mM	0.80 mL	4.00 mL	8.01 mL
5 mM	0.40 mL	2.00 mL	4.00 mL
25 mM	0.08 mL	0.40 mL	0.80 mL

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References for AZD 9291

References are publications that support the biological activity of the product.

Cross AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 PMID: 24893891