CHMFL-PI3KD-317

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CHMFL-PI3KD-317

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2244992-76-3

包装与价格：

包装	价格(元)
10mg	电议
25mg	电议

产品介绍

CHMFL-PI3KD-317 是一种高效、选择性、可口服的 PI3Kδ 抑制剂，IC50 值为 6 nM，对其选择性是对其他 PIKK 家族的 10-1500 倍，例如 PI3Kα (IC50，62.6 nM)，PI3Kβ (IC50，284 nM)，PI3Kγ (IC50，202.7 nM)，PIK3C2A (IC50，>10000 nM)，PIK3C2B (IC50，882.3 nM)，VPS34 (IC50，1801.7 nM)，PI4KIIIA (IC50，574.1 nM) 和 PI4KIIIB (IC50，300.2 nM)。在 Raji 细胞中，CHMFL-PI3KD-317 抑制 PI3Kδ 介导的 Akt T308 磷酸化，EC50 值为 4.3 nM。CHMFL-PI3KD-317 对癌细胞具有抗增殖作用。

Cas No.

2244992-76-3

分子式

C₂₁H₂₄ClN₅O₃S₂

分子量

494.03

储存条件

Store at -20°C

General tips

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

产品描述

CHMFL-PI3KD-317 is a highly potent, selective and orally activePI3Kδinhibitor, with anIC₅₀of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC₅₀, 62.6 nM), PI3Kβ (IC₅₀, 284 nM), PI3Kγ (IC₅₀, 202.7 nM), PIK3C2A (IC₅₀, >10000 nM), PIK3C2B (IC₅₀, 882.3 nM), VPS34 (IC₅₀, 1801.7 nM), PI4KIIIA (IC₅₀, 574.1 nM) and PI4KIIIB (IC₅₀, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC₅₀of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells^[1].

CHMFL-PI3KD-317 has antiproliferative effects, with GI₅₀s of 3.5?±?0.8, 4.0?±?0.9, 4.8?±?0.2, 3.3?±?0.2, 3.0?±?0.4 μM against PF382, NALM-6, MV4-11, MOLM-14 and MOLM-13 cells, respectively^[1].

CHMFL-PI3KD-317 (Compound 15i; 25, 50 and 100?mg/kg/day, p.o., for 14 days) inhibits the growth of the MOLM14 tumor in mice^[1].
CHMFL-PI3KD-317 shows favorable oral bioavailability and acceptable half-life (T_1/2?=?3.28?h) in Sprague-Dawley rats^[1].

Animal Model:	Female nu/nu mice bearing MOLM-14 tumor xenografts^[1]
Dosage:	25, 50 and 100?mg/kg/day
Administration:	P.O. for 14 days
Result:	Inhibited the growth of the MOLM14 tumor without mortality or obvious weight loss in mice.