PI3Kδ-IN-10
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.
- CAS No.: 2409725-49-9
- Formula: C19H16ClN9
- Molecular Weight:405.84
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PI3Kδ 2 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Bel-7402 | IC50 |
1.36 μM
Compound: 9x
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Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
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[PMID: 35191698] |
| Hep 3B2 | IC50 |
1.09 μM
Compound: 9x
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Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
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[PMID: 35191698] |
| HepG2 | IC50 |
0.53 μM
Compound: 9x
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Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
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[PMID: 35191698] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Bel-7402, HepG2, Hep3B[1]
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Concentration:0-10 μM
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Incubation Time:72 hours
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Result:Showed cell proliferation inhibitory effects in HCC cell lines with IC50 of 0.53 - 1.36 μM.
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Cell Line:Bel-7402, HepG2[1]
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Concentration:0 μM, 1.56 μM, 3.12 μM, 6.25 μM, 12.5 μM, 50 μM
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Incubation Time:24 hours
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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.
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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Balb/c (nu/nu) mice[1]
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Dosage:5 mg/kg or 1 mg/kg
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Administration:PO and IV, single (Pharmacokinetic Analysis)
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Result:Exhibited an acceptable half-life (T1/2), a moderate distribution volume, and acceptable oral bioavailability.
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Animal Model:Female Balb/c (nu/nu) mice (6 weeks)[1]
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Dosage:40 and 20 mg/kg
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Administration:IV, for 12 days
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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.
Chemical Information
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CAS No. 2409725-49-9
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Molecular Weight 405.84
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Formula C19H16ClN9
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SMILES
N#CC1=C(N[C@H](C2=NN(C3=CC=CN=C3)C4=C2C=CC(Cl)=C4)C)N=C(N)N=C1N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PI3Kδ-IN-10 Related Classifications
HY-144254 Related Classifications
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