XL-147

Background Information:

XL-147 (Pilaralisib) is a potent, selective and orally bioavailable
ATP-competitive small molecule inhibitor targeting pan-class I
phosphatidylinositol 3 kinase (PI3K) family with IC50 values of 39, 383,
36 and 23 nM for p110 α, β, δ and γ isoforms, and is highly selective
over mTOR (IC50 > 15000 nM), VPS34 (IC50 = 6975 nM), DNAPK (IC50 =
4750 nM). It is currently in clinical trials for cancer treatment.

Reference:

1. GI Shapiro, et al., Phase I safety, pharmacokinetic, and
pharmacodynamic study of SAR245408 (XL147), an oral pan-class I PI3K
inhibitor, in patients with advanced solid tumors. Clin Cancer Res. 2014
Jan 1;20(1):233-45. doi: 10.1158/1078-0432.CCR-13-1777.
2. CP Reynolds, et al., Initial testing (stage 1) of the
phosphatidylinositol 3′ kinase inhibitor, SAR245408 (XL147) by the
pediatric preclinical testing program. Pediatr Blood Cancer, 2013 May;
60(5):791-8. doi: 10.1002/pbc.24301.
3. L. Debussche, et al, Compositions comprising a pi3k inhibitor and a
mek inhibitor and their use for treating cancer, EP 2648729 A1 (text
from WO2012078832A1).

APIM050262: XL-147

CAS No.: 934526-89-3.
Molecular Formula: C₂₅H₂₅ClN₆O₄S•0.5HCl.
Molecular Weight: 559.3.
Purity: >99% (HPLC at 214 and 254 nm).
QC: HPLC-MS, ¹HNMR, Microanalysis (Elemental Analysis).
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.