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.
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- CAS No.: 2101518-75-4
- Formule: C28H21F2N7O
- Masse moléculaire:509.51
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
PI3Kδ 3.3 nM (IC50) |
PI3Kγ 17.9 nM (IC50) |
PI3Kβ 241.6 nM (IC50) |
PI3Kα 377.2 nM (IC50) |
Cellular Effect
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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] |
In Vitro
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. Further protocols information, click here.
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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.
In Vivo
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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Masse moléculaire 509.51
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PI3Kδ-IN-8 Related Classifications
HY-134472 Related Classifications
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