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KPT-9274 Sale

目录号 : GC14615

Orally acitve allosteric inhibitor of PAK4

KPT-9274 Chemical Structure

Cas No.:1643913-93-2

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥3,627.00
现货
5mg
¥2,352.00
现货
10mg
¥4,050.00
现货
50mg
¥11,700.00
现货
100mg
¥18,900.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

KPT-9274 is a selective and orally bioavailable allosteric inhibitor of PAK4 [1][2][3].

P21 protein (Cdc42/Rac)-activated kinase 4 (PAK4) is a serine/threonine-protein kinase and a member of the PAK family of proteins which are Rac1 and Cdc42 effectors. PAK4 is a mediator of filopodia formation and stabilizes β-catenin transcriptional activity, and is involved in disease progression for several solid tumors [1][2][3].

KPT-9274 is a selective and orally bioavailable PAK4 inhibitor. In MDA-MB-468 cells, KPT-9274 showed anti-tumor activity with IC50 value of 0.12 μM. KPT-9274 reduced PAK4 protein and the key downstream effectors of cell cycle (β-catenin, cyclin D1), cell migration (cofilin), autophagy (AMPK) and apoptosis (Caspase and PARP cleavage) [1]. In RCC cells, KPT-9274 dose-dependently inhibited cell viability [2]. In AML cell lines, KPT-9274 (1 nM-10 μM) inhibited cell proliferation in a dose-and time- dependent way and reduced protein and mRNA expression of PAK4 [3].

In mice inoculated with MDA-MB-231 or MDA-MB-468 cells, KPT-9274 were given orally once daily (5 or 7 days/week) without major toxicity. KPT-9274 induced a maximum TGI of ~55% and ~70% in MDA-MB-231 and MDA-MB-468 mice, respectively [1]. In subcutaneous xenograft mouse models, KPT-9274 inhibited RCC growth [2]. In human AML leukemia xenograft model, KPT-9274 (150 mg/kg) significantly inhibited tumor growth, prevented invasion of MV4-11 cells, and improved overall survival [3].

References:
[1].  Senapedis W, George R, McCauley D, et al. Preclinical Evaluation of Novel PAK4 Allosteric Modulators Against Triple Negative Breast Cancer.
[2].  Aboud OA, Senapedis W, Landesman Y, et al. Inhibition of PAK4 attenuates renal cell carcinoma (RCC) growth.
[3].  Mitchell S, Orwick S, Cannon M, et al. In Vitro and In Vivo Anti-Leukemic Effects of KPT-9274, a Reported PAK4 Allosteric Modulator, in Acute Myeloid Leukemia: Promising Results Justifying Further Development in This Disease. 57th Annual Meeting & Exposition. Orlando, FL December 5-8, 2015.

Chemical Properties

Cas No. 1643913-93-2 SDF
化学名 (1Z,2E)-3-(6-aminopyridin-2-yl)-N-((5-(4-(4,4-difluoropiperidine-1-carbonyl)phenyl)-7-(4-fluorophenyl)benzofuran-2-yl)methyl)acrylimidic acid
Canonical SMILES FC1=CC=C(C2=CC(C3=CC=C(C(N4CCC(F)(F)CC4)=O)C=C3)=CC5=C2OC(C/N=C(O)/C([H])=C([H])/C6=NC(N)=CC=C6)=C5)C=C1
分子式 C35H29F3N4O3 分子量 610.62
溶解度 ≥ 22.45mg/mL in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.6377 mL 8.1884 mL 16.3768 mL
5 mM 0.3275 mL 1.6377 mL 3.2754 mL
10 mM 0.1638 mL 0.8188 mL 1.6377 mL
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