N-(3-{2-[3-Fluoro-4-(4-methyl-piperazin-1-yl)-phenylamino]-7H-pyrrolo[2,3-d]pyrimidin-4-yloxy}-phenyl)-acrylamide Chemical Properties

Density 

1.365±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO:30.0(Max Conc. mg/mL);61.53(Max Conc. mM)

form 

A crystalline solid

pka

12.48±0.50(Predicted)

color 

White to off-white

InChIKey

UOFYSRZSLXWIQB-UHFFFAOYSA-N

SMILES

C(NC1=CC=CC(OC2N=C(NC3=CC=C(N4CCN(C)CC4)C(F)=C3)N=C3NC=CC3=2)=C1)(=O)C=C

N-(3-{2-[3-Fluoro-4-(4-methyl-piperazin-1-yl)-phenylamino]-7H-pyrrolo[2,3-d]pyrimidin-4-yloxy}-phenyl)-acrylamide Usage And Synthesis

Description

Avitinib is a pyrrolopyrimidine-based, irreversible inhibitor of the epidermal growth factor receptor (EGFR). It is selective for EGFR-active and T790M mutations, exhibiting a 298-fold increase in potency compared with wild-type EGFR. In a xenograft model, oral administration of 500 mg/kg avitinib was shown to result in complete remission of tumors with EGFR-active and T790M mutations.

Uses

Abivertinib is a pyrrolopyrimidine-based, irreversible inhibitor of the epidermal growth factor receptor (EGFR). Abivertinib synergistically strengthens anti-leukemia activity of venetoclax in acute myeloid leukemia in BTK-dependent manner.

in vivo

IC 50

EGFR L858R: 0.18 nM (IC₅₀); EGFR^T790M: 0.18 nM (IC₅₀); EGFR (WT): 7.68 nM (IC₅₀)

References

[1] XIAO XU. AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer Patients.[J]. Molecular Cancer Therapeutics, 2016, 15 11: 2586-2597. DOI: 10.1158/1535-7163.mct-16-0281

N-(3-{2-[3-Fluoro-4-(4-methyl-piperazin-1-yl)-phenylamino]-7H-pyrrolo[2,3-d]pyrimidin-4-yloxy}-phenyl)-acrylamide(1557267-42-1)Related Product Information

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