PI3Kδ-IN-8
PI3Kδ-IN-8 is a potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 3.3 nM. PI3Kδ-IN-8 shows selectivity for PI3Kδ over PI3Kα, PI3Kβ, and PI3Kγ (IC50=377.2, 241.6, 17.9 nM, respectively). PI3Kδ-IN-8 has anti-tumor activity.
For research use only. We do not sell to patients.
- CAS No.: 2101518-75-4
- Formula: C28H21F2N7O
- Molecular Weight:509.51
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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 3.3 nM (IC50) |
PI3Kγ 17.9 nM (IC50) |
PI3Kβ 241.6 nM (IC50) |
PI3Kα 377.2 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| OCI-Ly10 | ED50 |
6.47 mg/kg
Compound: 34
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Antitumor activity against human OCI-LY10 cells xenografted in orally dosed CB.17 SCID mouse assessed as tumor growth inhibition administered once daily for 24 days
Antitumor activity against human OCI-LY10 cells xenografted in orally dosed CB.17 SCID mouse assessed as tumor growth inhibition administered once daily for 24 days
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[PMID: 33297683] |
| OCI-Ly10 | IC50 |
<1 nM
Compound: 34
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Anticancer activity against human OCILY10 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay
Anticancer activity against human OCILY10 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay
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[PMID: 33297683] |
| SU-DHL-6 | IC50 |
<0.1 nM
Compound: 34
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Anticancer activity against human SUDHL-6 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay
Anticancer activity against human SUDHL-6 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay
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[PMID: 33297683] |
| TMD8 | ED50 |
5.45 mg/kg
Compound: 34
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Antitumor activity against human TMD-8 cells xenografted in orally dosed CB.17 SCID mouse assessed as tumor growth inhibition administered once daily for 24 days
Antitumor activity against human TMD-8 cells xenografted in orally dosed CB.17 SCID mouse assessed as tumor growth inhibition administered once daily for 24 days
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[PMID: 33297683] |
| TMD8 | IC50 |
<0.1 nM
Compound: 34
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Anticancer activity against human TMD8 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay
Anticancer activity against human TMD8 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay
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[PMID: 33297683] |
PI3Kδ-IN-8 (compound 34) (0.1 nM-10 μM; 96 h) shows excellent potency against representative DLBCL cell lines, of either GCB (SUDHL-6), or ABC subtype (OCI-Ly10 and TMD-8)[1].
PI3Kδ-IN-8 (1 h) inhibits the PI3K-induced AKT phosphorylation in anti-IgM stimulated Raji cells, with an IC50 of 9.5 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SUDHL-6, OCI-Ly10, and TMD-8 cell lines
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Concentration:0.1, 1, 10, 100, 1000, 10000 nM
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Incubation Time:96 hours
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Result:Inhibited the viability of SUDHL-6, OCI-Ly10, and TMD-8 cells, with IC50s of <0.1 nM, <1 nM, and <0.1 nM, respectively.
PI3Kδ-IN-8 (1 mg/kg; i.v.) displays a suitable half-life (1 h), Cmax (2.3 μM) and low clearance (5.6 mL/min/kg) in mice[1].
PI3Kδ-IN-8 (10 mg/kg; p.o.) displays moderate oral bioavailability (39%), Cmax (7.5 μM), and AUClast(22 μM•h) in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female NOD scid mice were injected OCI-Ly10 cells[1]
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Dosage:1, 3, 10, 30 mg/kg
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Administration:P.o. once daily for 24 days
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Result:Reduced the tumor volume, with an ED50 of 6.47 mg/kg.
Tumor growth inhibition of 81.95% was seen with a highly significant reduction in both tumor volume and tumor weight.
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Animal Model:Male BALB/c mice[1]
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Dosage:1 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis)
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Administration:Intravenous administration and oral administration
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Result:I.v.: t1/2=1 h, Cmax=2.3 μM, CL=5.6 mL/min/kg.
P.o.: F=39%, Cmax=7.5 μM, AUClast=22μM•h.
Chemical Information
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CAS No. 2101518-75-4
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Molecular Weight 509.51
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Formula C28H21F2N7O
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SMILES
N#CC1=C(N[C@H](C(C(C2=CC=C(F)C=C2)=C3C=CC(F)=CN43)=C(C5=CC=CC=C5)C4=O)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-8 Related Classifications
HY-134472 Related Classifications
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