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.

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PI3Kδ/γ-IN-3

PI3Kδ/γ-IN-3 構造式

CAS 番号 : 2730151-31-0

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PI3Kδ/γ-IN-3 関連抗体

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PI3K アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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製品説明

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)

Cellular Effect
Cell Line Type Value Description References
DOHH-2 IC50
0.2 μM
Compound: 58
Antiproliferative activity against human DOHH-2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human DOHH-2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 35831917]
SU-DHL-6 IC50
0.06 nM
Compound: 58
Antiproliferative activity against human SUDHL2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human SUDHL2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 35831917]
SU-DHL-6 IC50
0.06 μM
Compound: 58
Antiproliferative activity against human SU-DHL-6 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human SU-DHL-6 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 35831917]
SUD4 IC50
0.03 μM
Compound: 58
Antiproliferative activity against human SU-DHL-4 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human SU-DHL-4 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 35831917]
体外実験

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 関連抗体

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.
体内実験

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
分子量

473.92

分子式

C23H20ClN9O
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
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PI3Kδ/γ-IN-3 Related Classifications

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  • 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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製品番号:
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