PF-4989216 - CAS 1276553-09-3
Catalog number: 1276553-09-3
Category: Inhibitor
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Molecular Formula:
C18H13FN6OS
Molecular Weight:
380.401
COA:
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Targets:
PI3K
Description:
PF-4989216 is a novel potent and selective PI3K inhibitor. PF-4989216 inhibits the phosphorylation of PI3K downstream molecules and subsequently leads to inhibition in cell proliferation and xenograft tumor growth in NSCLCs harboring a PIK3CA mutation, including an erlotinib resistant line, NCI-H1975. Although PF-4989216 inhibits the phosphorylation of PI3K downstream molecules in the NSCLCs with PTEN loss (NCI-H1650), PF-4989216 does not sufficiently induce anti-tumor efficacy in NCI-H1650. PF-4989216 is a potential cancer drug candidate for erlotinib resistant non-small-cell lung cancer patients with PIK3CA mutation.
Synonyms:
PF-4989216; PF 4989216; PF4989216.
MSDS:
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InChIKey:
MUENOTXSRZEFJV-UHFFFAOYSA-N
InChI:
InChI=1S/C18H13FN6OS/c19-14-7-11(8-20)1-2-12(14)15-13(9-21)18(25-3-5-26-6-4-25)27-16(15)17-22-10-23-24-17/h1-2,7,10H,3-6H2,(H,22,23,24)
Canonical SMILES:
C1COCCN1C2=C(C(=C(S2)C3=NC=NN3)C4=C(C=C(C=C4)C#N)F)C#N
Current Developer:
Pfizer, Inc.
1.Targeting small cell lung cancer harboring PIK3CA mutation with a selective oral PI3K inhibitor PF-4989216.
Walls M1, Baxi SM, Mehta PP, Liu KK, Zhu J, Estrella H, Li C, Zientek M, Zong Q, Smeal T, Yin MJ. Clin Cancer Res. 2014 Feb 1;20(3):631-43. doi: 10.1158/1078-0432.CCR-13-1663. Epub 2013 Nov 15.
PURPOSE: Constitutive activation of phosphoinositide 3-kinase (PI3K) occurs frequently in many human tumors via either gene mutation in the p110α catalytic subunit of PI3K or functional loss of tumor suppressor PTEN. Patients with small-cell lung cancer (SCLC) have very poor prognosis and survival rates such that an effective targeted therapy is in strong demand for these patients. In this study, we characterized the highly selective oral PI3K inhibitor, PF-4989216, in preclinical SCLC models to investigate whether targeting the PI3K pathway is an effective targeted therapy option for SCLCs that harbor a PIK3CA mutation.
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CAS 1276553-09-3 PF-4989216

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