CHMFL-PI3KD-317

生物活性靶点体外研究体内研究 CHMFL-PI3KD-317 试剂级价格

CHMFL-PI3KD-317

CAS号:2244992-76-3
英文名:CHMFL-PI3KD-317
中文名:CHMFL-PI3KD-317
CBNumber:CB54844643
分子式:C21H24ClN5O3S2
分子量:494.03
MOL File:2244992-76-3.mol

CHMFL-PI3KD-317化学性质

密度 :1.406±0.06 g/cm3(Predicted)
储存条件 :Store at -20°C
酸度系数(pKa) :6.25±0.50(Predicted)

CHMFL-PI3KD-317性质、用途与生产工艺

生物活性 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。

靶点

PI3Kδ

6 nM (IC ₅₀ )

PI3Kα

62.6 nM (IC ₅₀ )

PI3Kβ

284 nM (IC ₅₀ )

PI3Kγ

202.7 nM (IC ₅₀ )

PIK3C2B

882.3 nM (IC ₅₀ )

Vps34

1801.7 nM (IC ₅₀ )

PI4KIIIA

574.1 nM (IC ₅₀ )

PI4KIIIB

300.2 nM (IC ₅₀ )

体外研究

CHMFL-PI3KD-317 has antiproliferative effects, with GI ₅₀ s 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.

体内研究

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 (T _1/2 = 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.