2. PI3K/Akt/mTOR
  3. PI3K
  4. PI3Kδ-IN-8

PI3Kδ-IN-8 是一种有效，选择性和具有口服活性的 PI3Kδ 抑制剂，IC50 值为 3.3 nM。PI3Kδ-IN-8 对 PI3Kδ 的选择性超过 PI3Kα，PI3Kβ，PI3Kγ (IC50=377.2, 241.6, 17.9 nM)。PI3Kδ-IN-8 具有抗肿瘤活性。

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PI3Kδ-IN-8 Chemical Structure

PI3Kδ-IN-8 Chemical Structure

CAS No. : 2101518-75-4

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PI3Kδ-IN-8 相关抗体

Top Publications Citing Use of Products

查看 PI3K 亚型特异性产品:

查看所有亚型
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].

IC50 & Target[1]

PI3Kδ

3.3 nM (IC50)

PI3Kγ

17.9 nM (IC50)

PI3Kβ

241.6 nM (IC50)

PI3Kα

377.2 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
OCI-Ly10 IC50
< 1 nM
Compound: 34
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
[PMID: 33297683]
OCI-Ly10 ED50
6.47 mg/kg
Compound: 34
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
[PMID: 33297683]
SU-DHL-6 IC50
< 0.1 nM
Compound: 34
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
[PMID: 33297683]
TMD8 IC50
< 0.1 nM
Compound: 34
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
[PMID: 33297683]
TMD8 ED50
5.45 mg/kg
Compound: 34
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
[PMID: 33297683]
体外研究
(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].

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

PI3Kδ-IN-8 相关抗体:

Cell Viability Assay[1]

Cell Line: SUDHL-6, OCI-Ly10, and TMD-8 cell lines
Concentration: 0.1, 1, 10, 100, 1000, 10000 nM
Incubation Time: 96 hours
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.
体内研究
(In Vivo)

PI3Kδ-IN-8 (1-30 mg/kg; p.o. once daily for 24 d) significantly reduces the tumor volume and tumor weight in a dose-dependent manner in mice[1].
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].

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

Animal Model: Female NOD scid mice were injected OCI-Ly10 cells[1]
Dosage: 1, 3, 10, 30 mg/kg
Administration: P.o. once daily for 24 days
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.
Animal Model: Male BALB/c mice[1]
Dosage: 1 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
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.
分子量

509.51

Formula

C28H21F2N7O
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-8 相关分类

  • 摩尔计算器

  • 稀释计算器

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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-82101518-75-4PI3KPhosphoinositide 3-kinasePI3Kδanti-tumorcancerInhibitorinhibitorinhibit

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