2. PI3K/Akt/mTOR
  3. PI3K
  4. IHMT-PI3K-455

IHMT-PI3K-455 (Compound 15u) 是一种有效，选择性和具有口服活性的 PI3Kγ/δ 双重抑制剂。IHMT-PI3K-455 对 PI3Kγ 和 PI3Kδ 的 IC50 分别为 7.1 nM 和 0.57 nM。IHMT-PI3K-455 抑制了 AKT 磷酸化。IHMT-PI3K-455 通过招募和激活更多 CD8+ 杀伤 T 细胞抑制肿瘤生长。IHMT-PI3K-455 可用于肿瘤研究。

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IHMT-PI3K-455 Chemical Structure

IHMT-PI3K-455 Chemical Structure

CAS No. : 3047746-40-4

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IHMT-PI3K-455 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

IHMT-PI3K-455 (Compound 15u) is a potent, selective, orally active PI3Kγ/δ dual inhibitor with IC50s of 7.1 nM and 0.57 nM for PI3Kγ and PI3Kδ, respectively. IHMT-PI3K-455 suppresses the AKT phosphorylation. IHMT-PI3K-455 inhibits tumor growth by recruiting and activating more CD8+ killing T cells.IHMT-PI3K-455 is used in cancer research[1].

IC50 & Target

PI3Kα

6.717 μM (IC50)

PI3Kβ

42.04 nM (IC50)

PI3Kγ

7.1 nM (IC50)

PI3Kδ

0.57 nM (IC50)

体外研究
(In Vitro)

IHMT-PI3K-455 (1 μM，2 小时) 抑制了 RAW264.7 和 Raji 细胞中 PI3Kγ/δ 介导的 AKT 磷酸化[1]。
IHMT-PI3K-455 (1 μM，72 小时) 改变由 THP-1 和 BMDM 细胞衍生的 M2 巨噬细胞的极化[1]。

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

IHMT-PI3K-455 相关抗体:

Cell Differentiation Assay[1]

Cell Line: Macrophages
Concentration: 0.1, 1 μM
Incubation Time: 72 h
Result: Increased the proinflammatory M1 macrophage phenotype in a dose-dependent manner, with a concomitant dose-dependent decrease of the anti-inflammatory M2 macrophage phenotype.
Repolarized M2 phenotype toward M1 phenotype in THP-1 and BMDM macrophages.

Western Blot Analysis[1]

Cell Line: RAW264.7 cells; Raji cells
Concentration: 0, 0.01, 0.03, 0.1, 0.3, 1 μM
Incubation Time: 2 h
Result: Potently inhibited the PI3Kγ-mediated AKT473 phosphorylation in RAW264.7 cells (human C5a stimulation) with an IC50 value of 0.015 μM.
Potently inhibited the PI3Kδ-mediated AKT473 phosphorylation in Raji cells (anti-IgM stimulation) with an IC50 value of 0.010 μM.
体内研究
(In Vivo)

IHMT-PI3K-455 (40 mg/kg，口服；一天一次，连用 30 天) 抑制了 MC38 肿瘤异种移植模型中的肿瘤生长[1]。
IHMT-PI3K-455 (40 mg/kg，口服；一天一次，连用 30 天) 通过招募和激活更多 CD8+ 杀伤 T 细胞抑制肿瘤生长[1]。
Pharmacokinetic parameters of IHMT-PI3K-455 in Sprague-Dawley rats[1]

Dose (mg/kg) Administration route Cmax (ng/mL) Tmax (h) AUC0-∞ (h ng/mL) T1/2 (h) CL (L/h/kg) Vz (L/kg) F (%)
1 i.v. 1233 0.03 477 1.59 2.12 4.80 -
10 p.o. 157 3.42 838 2.71 14.76 56.02 17.6

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

Animal Model: MC38 tumor model[1]
Dosage: 10 mg/kg, 40 mg/kg
Administration: Oral gavage (p.o.); Once daily for 30 days
Result: Significantly inhibited tumor size in a dose-dependent manner.
Increased tumor-infiltrating CD8+T cells.
分子量

517.49

Formula

C26H21F2N7O3
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

IHMT-PI3K-455 相关分类

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  • 稀释计算器

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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:

IHMT-PI3K-4553047746-40-4PI3KPhosphoinositide 3-kinaseCancerMC38 xenograft modelTHP-1BMDM macrophagesInhibitorinhibitorinhibit

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