2. PI3K/Akt/mTOR
  3. PI3K
  4. PI3Kδ/γ-IN-2

PI3Kδ/γ-IN-2 is a potent PI3Kδ and PI3Kγ dual inhibitor with IC50s of 1 nM and 4.3 nM, respectively. PI3Kδ/γ-IN-2 has favorable oral bioavailability. PI3Kδ/γ-IN-2 has potential for battling B-cell malignancies.

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PI3Kδ/γ-IN-2 Chemical Structure

PI3Kδ/γ-IN-2 Chemical Structure

CAS No. : 2412195-89-0

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PI3Kδ/γ-IN-2 Related Antibodies

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Description

PI3Kδ/γ-IN-2 is a potent PI3Kδ and PI3Kγ dual inhibitor with IC50s of 1 nM and 4.3 nM, respectively. PI3Kδ/γ-IN-2 has favorable oral bioavailability. PI3Kδ/γ-IN-2 has potential for battling B-cell malignancies[1].

IC50 & Target[1]

PI3Kδ

1 nM (IC50)

PI3Kγ

4.3 nM (IC50)

In Vitro

PI3Kδ/γ-IN-2 (compound 26) (0-5 μM; 72 hours) exhibits remarkable anti-proliferative activity against SU-DHL-6 cell line[1].
PI3Kδ/γ-IN-2 (10-100 nM; 2 hours) down-regulates both phos-Akt (Ser473) and phos-S6K1 (Thr389), and decreases the phosphoration of Akt and S6K1 at 30 nM[1].

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

PI3Kδ/γ-IN-2 Related Antibodies

Cell Proliferation Assay

Cell Line: SU-DHL-6[1]
Concentration: 0-5 μM
Incubation Time: 72 hours
Result: Exhibited remarkable anti-proliferative activity against SU-DHL-6 cell line with GI50 value of 33 nM.

Western Blot Analysis

Cell Line: SU-DHL-6[1]
Concentration: 10, 30 and 100 nM
Incubation Time: 2 hours
Result: Down-regulated both phos-Akt (Ser473) and phos-S6K1 (Thr389) in a dose-dependent manner, and exhibited a more significant decrease in the phosphoration of Akt and S6K1 at 30 nM.
In Vivo

PI3Kδ/γ-IN-2 (5 mg/kg; PO or IV; single) exhibits a high plasma exposure, an attractive oral bioavailability, and an acceptable clearance[1].
Pharmacokinetic Parameters of PI3Kδ/γ-IN-2 in male Sprague-Dawley rats[1].

IV (5 mg/kg) PO (5 mg/kg)
T1/2 (h) 3.0 ± 0.3 14.3 ± 4.4
AUC0-t (h·μg/L) 5576 ± 606 4878 ± 694
VSS (L/kg) 3.9 ± 0.6
CL (L/h/kg) 0.9 ± 0.1
F (%) 87.5 ± 12.5

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

Animal Model: Male Sprague-Dawley rats[1]
Dosage: 5 mg/kg
Administration: PO or IV; single (Pharmacokinetics Analysis)
Result: Exhibited a high plasma exposure (AUC0-t = 4878 ± 694 h μg/L), an attractive oral bioavailability (F% = 87.5 ± 12.5), and an acceptable clearance (CL = 0.9 ± 0.1 L/h/kg).
Molecular Weight

484.94

Formula

C25H21ClN8O
CAS No.
SMILES

N#CC1=C(N=C(N=C1N2CC3(C[C@H]2C4=NC5=CC=CC(Cl)=C5C(N4C6=CC=CC=C6)=O)CC3)N)N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PI3Kδ/γ-IN-2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PI3Kδ/γ-IN-22412195-89-0PI3KPhosphoinositide 3-kinaseB-cell malignanciesAnticancerOral bioavailabilitySU-DHL-6Inhibitorinhibitorinhibit

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