PI3Kδ-IN-10_product_DataBase

Bioactivity	PI3Kδ-IN-10 is a highly potent and orally active PI3Kδ inhibitor with IC50 of 2 nM. PI3Kδ-IN-10 robustly suppresses the downstream AKT pathway to induce subsequent apoptosis in hepatocellular carcinoma models[1].
Invitro	PI3Kδ-IN-10 (compound 9x) (0-10 μM; 72 hours) has cell proliferation inhibitory effects in HCC cell lines with IC50 of 0.53 - 1.36 μM[1].PI3Kδ-IN-10 (0-50 μM; 24 hours) markedly enhances expression level of cleaved PARP and cleaved caspase-3, also reduces the level of Akt phosphorylation at Ser473 and Thr308 in a dose-dependent manner[1]. Cell Proliferation Assay Cell Line:
In Vivo	PI3Kδ-IN-10 (5 mg/kg for PO, 1 mg/kg for IV, single) exhibits an acceptable half-life (T1/2), a moderate distribution volume, and acceptable oral bioavailability[1].PI3Kδ-IN-10 (40 and 20 mg/kg; IV, for 12 days) effectively suppress the growth of live cancer xenografts with inhibition ratios of 76.02% and 59.15% at 40 mg/kg and 20 mg/kg[1].Pharmacokinetic Parameters of PI3Kδ-IN-10 in female Balb/c (nu/nu) mice[1].
Name	PI3Kδ-IN-10
CAS	2409725-49-9
Formula	C19H16ClN9
Molar Mass	405.84
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Qi J, Wang W, Tang Y, et al. Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma. J Med Chem. 2022;65(5):3849-3865.

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