Pilaralisib

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP01861CAS No. ：956958-53-5Purity：98%

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CAS No.	956958-53-5	Cat. No.	BCP01861
Name	Pilaralisib
Synonyms	SAR245408;XL-147;SAR 245408;XL 147;SAR-245408;
SMILES
Chemical Name
Formula	C21H16N6O2S2	M. Wt	448.52
Purity	98%	Storage	Store at 4-8°C
Description	XL147 inhibits class I PI3K isoforms in an ATP-competitive manner. In a panel of HER2-overexpressing human breast cancer cell lines, treatment with XL147 abrogates AKT and S6 phosphorylation but also induces the expression and phosphorylation of HER3 and other RTKs. In HER2+ cells, phosphorylation of HER3 is maintained by the HER2 tyrosine kinase, leading to partial recovery of phosphorylated AKT (pAKT) and thereby limiting the antitumor action of XL 147. In addition, knockdown of HER3 or treatment with the anti-HER2 agents trastuzumab or lapatinib sensitizes HER2+ breast cancer cells to XL147 in vitro and in vivo. Treatment with XL147 inhibits the monolayer growth of all tested cell lines, including BT474, HCC1937 et al. in a dose-dependent manner. The main effect of XL147 is inhibition of cell proliferation. XL147 induces cell death at the concentration of 20 μM. Treatment with XL147 leads to dose-dependent inhibition of PI3K. Consistent with the inhibition of cell proliferation, XL1