1676893-24-5
|
|
|
- CAS号:
- 1676893-24-5
- 英文名:
- NSC781406
- 英文别名:
- NSC781406;NSC-781406;NSC 781406;NSC781406;NSC-781406;NSC 781406;NSC781406,Phosphoinositide 3-kinase,NSC 781406,NSC-781406,PI3K,Mammalian target of Rapamycin,Inhibitor,inhibit,mTOR;Benzenesulfonamide, 2,4-difluoro-N-[2-methoxy-5-[4-[3-[4-(methylsulfonyl)-1-piperazinyl]-1-propyn-1-yl]-6-quinolinyl]-3-pyridinyl]-
- 中文名:
- 1676893-24-5
- 中文别名:
- 化合物NSC781406;PI3K和MTOR抑制剂(NSC781406)
- CBNumber:
- CB43334188
- 分子式:
- C29H27F2N5O5S2
- 分子量:
- 627.68
- MOL File:
- 1676893-24-5.mol
|
|
|
1676893-24-5化学性质
-
沸点:
-
775.1±70.0 °C(Predicted)
-
|
-
密度:
-
1.52±0.1 g/cm3(Predicted)
-
|
-
储存条件:
-
Store at -20°C
-
|
-
溶解度:
-
DMF: 10mg/mL; DMSO: 20mg/mL; DMSO:PBS (pH 7.2) (1:4): 0.2mg/mL
-
|
-
形态:
-
A solid
-
|
-
酸度系数(pKa):
-
6.23±0.40(Predicted)
-
|
1676893-24-5性质、用途与生产工艺
NSC781406是高效的 PI3K 和 mTOR 抑制剂，对PI3Kα的 IC50 值为2 nM。
|
PI3Kα
2 nM (IC
50
)
|
PI3Kγ
2.7 nM (IC
50
)
|
PI3Kβ
9.4 nM (IC
50
)
|
PI3Kδ
14 nM (IC
50
)
|
mTOR
5.4 nM (IC
50
)
|
NSC781406 demonstrates potent PI3K inhibition (PI3Kα IC
50
=2.0 nM) that translates into BEL-7404 cells proliferation inhibition (IC
50
=20 nM). NSC781406 displays reasonable liver microsome stability. NSC781406 demonstrates cytotoxic activities against leukemia, non-small cell, lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, and breast cancer. It is potent against 60 cancer cell lines with a mean GI
50
value of 65 nM, and with a GI50 value less than 10 nM against four cancer cell lines.
In the xenograft models, treatment with 30 mg/kg of NSC781406 results in statistically significant antitumor activity, with a mean reduction in relative tumor volume ratio of 52%. Sorafenib displays an inhibition ratio of 44% at 50 mg/kg. NSC781406 is well tolerated at 30 mg/kg, with no observed mortality or significant reduction of body weight.
1676893-24-5
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-100470 | 1676893-24-5
NSC781406 | 1676893-24-5 | 1mg | 600元 |
| 2024/04/30 | HY-100470 | 1676893-24-5
NSC781406 | 1676893-24-5 | 10mM * 1mLin DMSO | 1660元 |
1676893-24-5, 1676893-24-5 相关搜索:
- 细胞生物学试剂
- C29H27F2N5O5S2
- 化合物NSC781406
- PI3K和MTOR抑制剂(NSC781406)
- 1676893-24-5
- NSC781406,Phosphoinositide 3-kinase,NSC 781406,NSC-781406,PI3K,Mammalian target of Rapamycin,Inhibitor,inhibit,mTOR
- Benzenesulfonamide, 2,4-difluoro-N-[2-methoxy-5-[4-[3-[4-(methylsulfonyl)-1-piperazinyl]-1-propyn-1-yl]-6-quinolinyl]-3-pyridinyl]-
- NSC-781406;NSC 781406
- NSC781406;NSC-781406;NSC 781406
- NSC781406