CHMFL-PI3KD-317
|
|
|
- CAS号:
- 2244992-76-3
- 英文名:
- CHMFL-PI3KD-317
- 英文别名:
- CHMFL-PI3KD-317;CHMFL-PI-3KD-317,CHMFLPI3KD317,CHMFL PI3KD 317;Butanamide, 2-amino-N-[5-[6-chloro-5-[[(3-methylphenyl)sulfonyl]amino]-3-pyridinyl]-4-methyl-2-thiazolyl]-3-methyl-, (2S)-
- 中文名:
- CHMFL-PI3KD-317
- 中文别名:
- 化合物 T10804;化合物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
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。
|
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
)
|
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.
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.
|
CHMFL-PI3KD-317
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-112608 | CHMFL-PI3KD-317 | | 1 mg | 1360元 |
| 2024/04/30 | HY-112608 | CHMFL-PI3KD-317
CHMFL-PI3KD-317 | 2244992-76-3 | 5 mg | 3400元 |
2244992-76-3, CHMFL-PI3KD-317 相关搜索:
- 化合物CHMFL-PI3KD-317
- 化合物 T10804
- 2244992-76-3
- Butanamide, 2-amino-N-[5-[6-chloro-5-[[(3-methylphenyl)sulfonyl]amino]-3-pyridinyl]-4-methyl-2-thiazolyl]-3-methyl-, (2S)-
- CHMFL-PI-3KD-317,CHMFLPI3KD317,CHMFL PI3KD 317
- CHMFL-PI3KD-317