ChemicalBook > CAS DataBase List > N-(3-((2-((3-Fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide maleate

N-(3-((2-((3-Fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide maleate

Product Name: N-(3-((2-((3-Fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide maleate
CAS No.: 1557268-88-8
Chemical Name: N-(3-((2-((3-Fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide maleate
Synonyms: AC0010;AC-0010;AC 0010.;Avitinib (maleate);Avitinib (AC0010) maleate;Abivertinib maleate Avitinib;Avitinib maleate, 10 mM in DMSO;AC0010MA; AC-0010MA; AC 0010MA; AC0010; AC-0010; AC 0010.;N-(3-((2-((3-Fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide maleate;HER1,Abivertinib,EGFR,Inhibitor,Avitinib,AC0010,Epidermal growth factor receptor,Avitinib maleate,inhibit,ErbB-1,AC-0010,AC 0010
CBNumber: CB93161956
Molecular Formula: C30H30FN7O6
Formula Weight: 603.6009032
MOL File: 1557268-88-8.mol

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N-(3-((2-((3-Fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide maleate Property

storage temp.: Store at -20°C
solubility: DMSO:100.0(Max Conc. mg/mL);165.67(Max Conc. mM)
form: Solid
color: Light yellow to yellow

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-6952
Product name: Avitinibmaleate
Purity: 99.17%
Packaging: 5mg
Price: $84
Updated: 2021/12/16

ChemScene

Product number: CS-6952
Product name: Avitinibmaleate
Purity: 99.17%
Packaging: 10mg
Price: $144
Updated: 2021/12/16

ChemScene

Product number: CS-6952
Product name: Avitinibmaleate
Purity: 99.17%
Packaging: 50mg
Price: $540
Updated: 2021/12/16

ChemScene

Product number: CS-6952
Product name: Avitinibmaleate
Purity: 99.17%
Packaging: 100mg
Price: $780
Updated: 2021/12/16

Crysdot

Product number: CD11247354
Product name: N-(3-((2-((3-Fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamidemaleate
Purity: 97%
Packaging: 50mg
Price: $461
Updated: 2021/12/16

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N-(3-((2-((3-Fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide maleate Chemical Properties,Usage,Production

Uses

Avitinib (Abivertinib) maleate is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib maleate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate shows anticancer effects[1][2].

in vivo

Avitinib (AC0010; 12.5-500 mg/kg; orally administration; once daily; for 14 days) maleate 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 50

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

References

[1] Xu X, et al. AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer Patients. Mol Cancer Ther. 2016 Nov;15(11):2586-2597. DOI:10.1158/1535-7163.MCT-16-0281
[2] Yan X, et al. Promising efficacy of novel BTK inhibitor AC0010 in mantle cell lymphoma. J Cancer Res Clin Oncol. 2018;144(4):697-706. DOI:10.1007/s00432-017-2570-8

N-(3-((2-((3-Fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide maleate Preparation Products And Raw materials

Raw materials

Preparation Products

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1557268-88-8, N-(3-((2-((3-Fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide maleateRelated Search:

AC 0010.

AC0010

AC-0010

AC0010MA; AC-0010MA; AC 0010MA; AC0010; AC-0010; AC 0010.

Avitinib (maleate)

N-(3-((2-((3-Fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide maleate

2-Propenamide, N-[3-[[2-[[3-fluoro-4-(4-methyl-1-piperazinyl)phenyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]oxy]phenyl]-, (2Z)-2-butenedioate (1:1)

Avitinib (AC0010) maleate

HER1,Abivertinib,EGFR,Inhibitor,Avitinib,AC0010,Epidermal growth factor receptor,Avitinib maleate,inhibit,ErbB-1,AC-0010,AC 0010

Abivertinib maleate Avitinib

Avitinib maleate, 10 mM in DMSO

1557268-88-8

C26H26FN7O2C4H4O4