CHMFL-PI3KD-317

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

CHMFL-PI3KD-317 

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。

CHMFL-PI3KD-317

CHMFL-PI3KD-317 Chemical Structure

CAS No. : 2244992-76-3

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10 mg ¥5400 询问价格 & 货期
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生物活性

CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 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 EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells[1].

IC50 & Target

PI3Kδ

6 nM (IC50)

PI3Kα

62.6 nM (IC50)

PI3Kβ

284 nM (IC50)

PI3Kγ

202.7 nM (IC50)

PIK3C2B

882.3 nM (IC50)

Vps34

1801.7 nM (IC50)

PI4KIIIA

574.1 nM (IC50)

PI4KIIIB

300.2 nM (IC50)

体外研究
(In Vitro)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

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 (T1/2 = 3.28 h) in Sprague-Dawley rats[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

494.03

Formula

C21H24ClN5O3S2

CAS 号

2244992-76-3

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.

参考文献
  • [1]. Liang X, et al. Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. Eur J Med Chem. 2018 Aug 5;156:831-846.

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