XL-147 derivative 2 (CAS 956958-53-5)
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XL147 is an ATP-competitive inhibitor of class I PI3K isoforms. XL147 abrogates Akt and S6 phosphorylation in HER2+ cells and also induces the expression and phosphorylation of HER3 and other RTKs. Treatment with the anti-HER2 agents trastuzumab or lapatinib sensitizes HER2+ breast cancer cells to XL147 in vitro. Treatment with XL147 inhibits the monolayer growth of all tested cell lines, including BT474, HCC1937 et al. in a dose-dependent manner. XL147 induces cell death at a concentration of 20 μM by inducing a reduction in cyclin D1 and pRB and increasing in levels of the CDK inhibitor p27KIPI. In HER2-overexpressing cells, inhibition of PI3K is followed by up-regulation of expression and phosphorylation of multiple receptor tyrosine kinases, including HER3
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
XL-147 derivative 2, 10 mg | sc-364658 | 10 mg | $265.00 | |||
XL-147 derivative 2, 50 mg | sc-364658A | 50 mg | $728.00 |