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

PI3Kδ/γ-IN-3 (Compound 58) is a potent and orally active PI3Kδ and PI3Kγ dual inhibitor with IC50s of 1 nM and 16 nM, respectively. PI3Kδ/γ-IN-3 induces tumor cell apoptosis and can be used for B-cell malignancies research.

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

PI3Kδ/γ-IN-3 Chemical Structure

PI3Kδ/γ-IN-3 Chemical Structure

CAS No. : 2730151-31-0

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PI3Kδ/γ-IN-3 Related Antibodies

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Description

PI3Kδ/γ-IN-3 (Compound 58) is a potent and orally active PI3Kδ and PI3Kγ dual inhibitor with IC50s of 1 nM and 16 nM, respectively. PI3Kδ/γ-IN-3 induces tumor cell apoptosis and can be used for B-cell malignancies research[1].

IC50 & Target

PI3Kδ

1 nM (IC50)

PI3Kγ

16 nM (IC50)

In Vitro

PI3Kδ/γ-IN-3 (Compound 58) (72 h) shows antiproliferative activity against B-cell lymphoma (DLBCL) cells[1].
PI3Kδ/γ-IN-3 (0.5 μM, 24 h) arrests cell cycle at G0/G1 phase in SUDHL-6 and DOHH2 cells[1].
PI3Kδ/γ-IN-3 (1.5 and 2 μM, 48 h) induces cell apoptosis in SUDHL-6 and DOHH2 cells[1].

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

PI3Kδ/γ-IN-3 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: SUDHL-4, SUDHL-6 and DOHH2 cells
Concentration:
Incubation Time: 72 h
Result: Showed antiproliferative activity with IC50s of 0.03 ± 0.03, 0.06 ± 0.01 and 0.20 ± 0.04 μM against SUDHL-4, SUDHL-6 and DOHH2 cells, respectively.

Cell Cycle Analysis[1]

Cell Line: SUDHL-6 and DOHH2 cells
Concentration: 0.5 μM
Incubation Time: Alone or in combination with Ibrutininb (HY-10997) (0.5 μM or 1 μM) for 24 h
Result: Caused a loss of G2/M phase cells and an increase in the percentage of cells in the G0/G1 phase. Induced cell cycle arrest alone or in combination with Ibrutinib in both cells.

Apoptosis Analysis[1]

Cell Line: SUDHL-6 and DOHH2 cells
Concentration: 1.5 μM and 2 μM
Incubation Time: Alone or in combination with Ibrutininb (1.5 μM or 1 μM) for 48 h
Result: Demonstrated the induction of apoptosis in both SUDHL-6 and DOHH2 cells, and the combination was stronger than treated alone.
In Vivo

PI3Kδ/γ-IN-3 (Compound 58) (5 and 10 mg/kg; p.o.; daily for 14d) suppresses the tumor volume in a dose-dependent manner without obvious toxicity in mice[1].

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

Animal Model: Female non obese diabetes/severe combined immunodeficient (NOD/SCID) mice, 6- to 8-week-old, SUDHL-6 xenograft model[1]
Dosage: 5 and 10 mg/kg alone or in combination with 10 mg/kg Ibrutinib
Administration: Oral administration, daily for 14 days
Result: Suppressed the tumor volume in a dose-dependent manner and demonstrated superior efficacy relative to Ibrutinib at 10 mg/kg QD administration. When in combination with Ibrutinib, showed greater tumor growth inhibitory effects.
Animal Model: SD rats[1]
Dosage: 5 mg/kg
Administration: Oral or intravenous administration (Pharmacokinetic Analysis)
Result: PK Profiles of PI3Kδ/γ-IN-3 (Compound 58) in Male SD Rats[1]
Compound dose (mg/kg) administration route Cmax (ng/mL) Tmax (h) AUC0-t (h•μg/L) T1/2 (h) CL (L/h/kg) Vss(L/kg) F (%)
58 5 oral 3637.81 3.33 8612.57 9.46 0.79 -- 126.5
5 intravenous 860.09 0.08 6806.92 2.79 0.75 2.86 --

PK profiles: Cmax, maximum plasma concentration; Tmax, tim
Molecular Weight

473.92

Formula

C23H20ClN9O
CAS No.
SMILES

O=C1N(C2=CN=CC=C2)C([C@H]3N(C4=NC(N)=NC(N)=C4C#N)[C@H](CC3)C)=NC5=CC=CC(Cl)=C51
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-3 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-32730151-31-0PI3KApoptosisPhosphoinositide 3-kinaseB-cell malignanciesDLBCLIbrutinibSUDHL-6DOHH2Inhibitorinhibitorinhibit

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