2. PI3K/Akt/mTOR Apoptosis
  3. PI3K Akt Apoptosis
  4. PI3Kδ-IN-10

PI3Kδ-IN-10 是一种高效且具有口服活性的 PI3Kδ 抑制剂，IC50 为 2 nM。PI3Kδ-IN-10 能在肝细胞癌模型中强烈抑制下游 AKT 通路，诱导后续细胞凋亡 (apoptosis)。

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PI3Kδ-IN-10 Chemical Structure

PI3Kδ-IN-10 Chemical Structure

CAS No. : 2409725-49-9

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PI3Kδ-IN-10 相关抗体

Top Publications Citing Use of Products

查看 PI3K 亚型特异性产品:

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Akt Akt1 Akt2 Akt3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PI3Kδ-IN-10 is a highly potent and orally active PI3Kδ inhibitor with IC50 of 2 nM. PI3Kδ-IN-10 robustly suppresses the downstream AKT pathway to induce subsequent apoptosis in hepatocellular carcinoma models[1].

IC50 & Target[1]

PI3Kδ

2 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Bel-7402 IC50
1.36 μM
Compound: 9x
Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
[PMID: 35191698]
Hep 3B2 IC50
1.09 μM
Compound: 9x
Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
[PMID: 35191698]
HepG2 IC50
0.53 μM
Compound: 9x
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
[PMID: 35191698]
体外研究
(In Vitro)

PI3Kδ-IN-10 (compound 9x) (0-10 μM; 72 hours) has cell proliferation inhibitory effects in HCC cell lines with IC50 of 0.53 - 1.36 μM[1].
PI3Kδ-IN-10 (0-50 μM; 24 hours) markedly enhances expression level of cleaved PARP and cleaved caspase-3, also reduces the level of Akt phosphorylation at Ser473 and Thr308 in a dose-dependent manner[1].

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

PI3Kδ-IN-10 相关抗体:

Cell Proliferation Assay

Cell Line: Bel-7402, HepG2, Hep3B[1]
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Showed cell proliferation inhibitory effects in HCC cell lines with IC50 of 0.53 - 1.36 μM.

Western Blot Analysis

Cell Line: Bel-7402, HepG2[1]
Concentration: 0 μM, 1.56 μM, 3.12 μM, 6.25 μM, 12.5 μM, 50 μM
Incubation Time: 24 hours
Result: Markedly enhanced expression level of cleaved PARP and cleaved caspase-3, also reduced the level of Akt phosphorylation at Ser473 and Thr308 in a dose-dependent manner.
体内研究
(In Vivo)

PI3Kδ-IN-10 (5 mg/kg for PO, 1 mg/kg for IV, single) exhibits an acceptable half-life (T1/2), a moderate distribution volume, and acceptable oral bioavailability[1].
PI3Kδ-IN-10 (40 and 20 mg/kg; IV, for 12 days) effectively suppress the growth of live cancer xenografts with inhibition ratios of 76.02% and 59.15% at 40 mg/kg and 20 mg/kg[1].
Pharmacokinetic Parameters of PI3Kδ-IN-10 in female Balb/c (nu/nu) mice[1].

PO (5 mg/kg) IV (1 mg/kg)
T1/2 (h) 2.502 1.131
AUC (h·μg/L) 3067.94 2791.37
Vz/F (L/kg) 6.15 0.587
Tmax (h) 3 0.083
F (%) 22.0

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

Animal Model: Female Balb/c (nu/nu) mice[1]
Dosage: 5 mg/kg or 1 mg/kg
Administration: PO and IV, single (Pharmacokinetic Analysis)
Result: Exhibited an acceptable half-life (T1/2), a moderate distribution volume, and acceptable oral bioavailability.
Animal Model: Female Balb/c (nu/nu) mice (6 weeks)[1]
Dosage: 40 and 20 mg/kg
Administration: IV, for 12 days
Result: Effectively suppressed the growth of live cancer xenografts with inhibition ratios of 76.02% and 59.15% at 40 mg/kg and 20 mg/kg.
分子量

405.84

Formula

C19H16ClN9
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PI3Kδ-IN-10 相关分类

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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-IN-102409725-49-9PI3KAktApoptosisPhosphoinositide 3-kinasePKBProtein kinase BPI3KδAKTHepatocellular carcinomaOrally activeBel-7402HepG2Inhibitorinhibitorinhibit

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