1. PI3K/Akt/mTOR
    Apoptosis
  2. PI3K
    Akt
    Apoptosis
  3. PI3Kδ-IN-10

PI3Kδ-IN-10 

Cat. No.: HY-144254
Handling Instructions

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.

For research use only. We do not sell to patients.

PI3Kδ-IN-10 Chemical Structure

PI3Kδ-IN-10 Chemical Structure

CAS No. : 2409725-49-9

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Description

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].

IC50 & Target[1]

PI3Kδ

2 nM (IC50)

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: Bel-7402, HepG2, Hep3B[1]
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Showed cell proliferation inhibitory effects in HCC cell lines with IC50 of 0.53 - 1.36 μM.

Western Blot Analysis

Cell Line: Bel-7402, HepG2[1]
Concentration: 0 μM, 1.56 μM, 3.12 μM, 6.25 μM, 12.5 μM, 50 μM
Incubation Time: 24 hours
Result: Markedly enhanced expression level of cleaved PARP and cleaved caspase-3, also reduced the level of Akt phosphorylation at Ser473 and Thr308 in a dose-dependent manner.
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].

PO (5 mg/kg) IV (1 mg/kg)
T1/2 (h) 2.502 1.131
AUC (h·μg/L) 3067.94 2791.37
Vz/F (L/kg) 6.15 0.587
Tmax (h) 3 0.083
F (%) 22.0

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Balb/c (nu/nu) mice[1]
Dosage: 5 mg/kg or 1 mg/kg
Administration: PO and IV, single (Pharmacokinetic Analysis)
Result: Exhibited an acceptable half-life (T1/2), a moderate distribution volume, and acceptable oral bioavailability.
Animal Model: Female Balb/c (nu/nu) mice (6 weeks)[1]
Dosage: 40 and 20 mg/kg
Administration: IV, for 12 days
Result: Effectively suppressed the growth of live cancer xenografts with inhibition ratios of 76.02% and 59.15% at 40 mg/kg and 20 mg/kg.
Molecular Weight

405.84

Formula

C19H16ClN9

CAS No.
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Storage

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PI3Kδ-IN-10
Cat. No.:
HY-144254
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