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1676893-24-5

中文名稱 1676893-24-5
英文名稱 NSC781406
CAS 1676893-24-5
分子式 C29H27F2N5O5S2
分子量 627.68
MOL 文件 1676893-24-5.mol
1676893-24-5 結(jié)構(gòu)式 1676893-24-5 結(jié)構(gòu)式

基本信息

中文別名
PI3K和MTOR抑制劑(NSC781406)
英文別名
NSC781406
NSC-781406
NSC 781406
NSC781406
NSC-781406
NSC 781406
Benzenesulfonamide, 2,4-difluoro-N-[2-methoxy-5-[4-[3-[4-(methylsulfonyl)-1-piperazinyl]-1-propyn-1-yl]-6-quinolinyl]-3-pyridinyl]-

物理化學(xué)性質(zhì)

沸點775.1±70.0 °C(Predicted)
密度1.52±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMF: 10mg/mL; DMSO: 20mg/mL; DMSO:PBS (pH 7.2) (1:4): 0.2mg/mL
酸度系數(shù)(pKa)6.23±0.40(Predicted)
形態(tài)固體
顏色White to off-white
1676893-24-5價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/08/19HY-1004701676893-24-5
NSC781406
1676893-24-55mg1037元
2024/08/19HY-1004701676893-24-5
NSC781406
1676893-24-510mM * 1mLin DMSO1432元
2024/08/19HY-1004701676893-24-5
NSC781406
1676893-24-510mg1660元

常見問題列表

生物活性
NSC781406是高效的 PI3K 和 mTOR 抑制劑,對PI3Kα的 IC50 值為2 nM。
靶點

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 )

體外研究

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.

體內(nèi)研究

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.

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