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
Chemenu
Product number
CM249788
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
1g
Price
$926
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); EGFRT790M: 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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N-(3-((2-((3-Fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide maleate Suppliers

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BOC Sciences
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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