A reversible class I PI3K inhibitor (IC50s = 39

XL147 – 5 mg

Brand:
Cayman
CAS:
934526-89-3
Storage:
-20
UN-No:
Non-Hazardous - /

The phosphatidylinositol 3-kinase (PI3K) signaling pathway has central roles in cell growth, development, and survival. XL147 is a methylbenzenesulfonamide derivative that reversibly inhibits class I PI3Ks (IC50s = 39, 36, 23, and 383 nM for p110α, δ, γ, and β, respectively).{29152} It has been shown to abrogate Akt and S6 kinase phosphorylation, reduce cyclin D1 and retinoblastoma protein, and upregulate the CDK inhibitor p27, inhibiting cell proliferation.{29152} In HER2-overexpressing breast cancer cells, cotreatment with the HER2 inhibitors trastuzumab or lapatinib (Item No. 11493) are reported to sensitize tumor cells to the growth inhibitory effect of XL147.{29153} This compound has been evaluated in clinical trials in patients with advanced solid tumors.{29154}  

 

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Description

A reversible class I PI3K inhibitor (IC50s = 39, 36, 23, and 383 nM for p110α, δ, γ, and β, respectively); inhibits HER2-overexpressing breast cancer cell proliferation

Formal name: 2-amino-N-[3-[[[3-[(2-chloro-5-methoxyphenyl)amino]-2-quinoxalinyl]amino]sulfonyl]phenyl]-2-methyl-propanamide

Synonyms:  Pilaralisib|SAR245408

Molecular weight: 541

CAS: 934526-89-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling

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