ChemicalBook > Product Catalog >Biochemical Engineering >Biochemical Reagents >Agonist Inhibitors >N-(3-{2-[3-Fluoro-4-(4-methyl-piperazin-1-yl)-phenylamino]-7H-pyrrolo[2,3-d]pyrimidin-4-yloxy}-phenyl)-acrylamide

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

N-(3-{2-[3-Fluoro-4-(4-methyl-piperazin-1-yl)-phenylamino]-7H-pyrrolo[2,3-d]pyrimidin-4-yloxy}-phenyl)-acrylamide Suppliers list
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N-(3-{2-[3-Fluoro-4-(4-methyl-piperazin-1-yl)-phenylamino]-7H-pyrrolo[2,3-d]pyrimidin-4-yloxy}-phenyl)-acrylamide Basic information
Product Name:N-(3-{2-[3-Fluoro-4-(4-methyl-piperazin-1-yl)-phenylamino]-7H-pyrrolo[2,3-d]pyrimidin-4-yloxy}-phenyl)-acrylamide
Synonyms:Avitinib;2-Propenamide, N-[3-[[2-[[3-fluoro-4-(4-methyl-1-piperazinyl)phenyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]oxy]phenyl]-;Avitinib(AC0010/AC0010MA);Avitinib free base;Avitinib (AC0010);N-(3-{2-[3-Fluoro-4-(4-methyl-piperazin-1-yl)-phenylamino]-7H-pyrrolo[2,3-d]pyrimidin-4-yloxy}-phenyl)-acrylamide;Avi Tini;CS-2348
CAS:1557267-42-1
MF:C26H26FN7O2
MW:487.53
EINECS:1592732-453-0
Product Categories:
Mol File:1557267-42-1.mol
N-(3-{2-[3-Fluoro-4-(4-methyl-piperazin-1-yl)-phenylamino]-7H-pyrrolo[2,3-d]pyrimidin-4-yloxy}-phenyl)-acrylamide Structure
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
pka12.48±0.50(Predicted)
color White to off-white
InChIKeyUOFYSRZSLXWIQB-UHFFFAOYSA-N
SMILESC(NC1=CC=CC(OC2N=C(NC3=CC=C(N4CCN(C)CC4)C(F)=C3)N=C3NC=CC3=2)=C1)(=O)C=C
Safety Information
MSDS Information
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
DescriptionAvitinib 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.
UsesAbivertinib 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

Avitinib (AC0010; 12.5-500 mg/kg; orally administration; once daily; for 14 days) inhibits EGFR-mutant tumor growth but not wild-type EGFR tumor growth in xenograft models over extended duration[1].

Animal Model:Nu/Nu nude mice (Six- to 8-week-old) injected with NCI-H1975 and A431 cells[1]
Dosage:12.5, 50, and 500 mg/kg
Administration:Orally administration; once daily; for 14 days
Result:Inhibited EGFR-mutant tumor growth but not wild-type EGFR tumor growth.
IC 50EGFR L858R: 0.18 nM (IC50); EGFRT790M: 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 Preparation Products And Raw materials
Tag: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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