Cat. No. Name Size Price Add Cart
KI3098XL-765 (SAR-245409)5 mg$336
XL-765 (SAR-245409)10 mg$592
XL-765 (SAR-245409)20 mg$538
XL-765 (SAR-245409)50 mg$1552
XL-765 (SAR-245409)100 mg$2482
XL-765 (SAR-245409)200 mg$3952
XL-765 (SAR-245409)1 g$15800

Chemical Characteristic

Product NameXL-765 (SAR-245409)
CAS No.1123889-87-1
Molecular Weight 599.66
FormulaC31H29N5O6S
Chemical Structure

Biological activities

XL765 is a potent and selective inhibitor of Class I PI3K isoforms and mTOR. The IC50s of XL765 against class I PI3K isoforms (p110α, β, γ and δ) are 39, 113, 9 and 43 nM, respectively. XL765 also inhibits DNA-PK and mTOR with IC50s of 150 and 157 nM閿涘espectively.[1] In vivo, in multiple human xenograft tumor models, XL765 inhibits PI3K pathway signaling leading to tumor growth inhibition or tumor shrinkage in a dose-dependent manner.[2]

Protocols

In vivo, XL765 is dissolved in DMSO.[2]

References

[1]Laird D. XL765 targets tumor growth, survival, and angiogenesis in preclinical models by dual inhibition of PI3K and mTOR. EORTC meeting. 2007.
[2]Papadopoulos K P, Markman B, Tabernero J, et al. A phase I dose-escalation study of the safety, pharmacokinetics (PK), and pharmacodynamics (PD) of a novel PI3K inhibitor, XL765, administered orally to patients (pts) with advanced solid tumors. J Clin Oncol (Meeting Abstracts). 2008, 26 (15_suppl): 3510.

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