CHMFL-PI3KD-317

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 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.

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.

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.CHMFL-PI3KD-317 shows favorable oral bioavailability and acceptable half-life (T1/2?=?3.28?h) in Sprague-Dawley rats.Animal Model:Female nu/nu mice bearing MOLM-14 tumor xenografts 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.

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PI3K/Akt/mTOR signaling

PI3K

PI3K | PI4K

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2244992-76-3

494.03

C21H24ClN5O3S2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (506.04 mM; 超声助溶 )

CC(C)[C@H](N)C(=O)Nc1nc(C)c(s1)-c1cnc(Cl)c(NS(=O)(=O)c2cccc(C)c2)c1

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(-20℃)

With Ice Pack

≥ 2 years