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174402-32-5

中文名稱 174402-32-5
英文名稱 Edotecarin
CAS 174402-32-5
分子式 C29H28N4O11
分子量 608.55
MOL 文件 174402-32-5.mol
174402-32-5 結(jié)構(gòu)式 174402-32-5 結(jié)構(gòu)式

基本信息

中文別名
化合物 T15200
英文別名
J 107088
PF 804950
Edotecarin
Edotecarin (J 107088)
5H-Indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione, 12-β-D-glucopyranosyl-12,13-dihydro-2,10-dihydroxy-6-[[2-hydroxy-1-(hydroxymethyl)ethyl]amino]-

物理化學(xué)性質(zhì)

熔點(diǎn)330° (dec)
比旋光度D23 +117° (c = 0.8 in 1:1 acetonitrile/water)
沸點(diǎn)1047.5±75.0 °C(Predicted)
密度1.96±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)9.61±0.20(Predicted)
形態(tài)Solid
顏色Yellow to orange

常見問題列表

生物活性
Edotecarin 是一種有效的 topoisomerase I 抑制劑,可誘導(dǎo)單鏈 DNA 斷裂,IC50 值為 50 nM。
靶點(diǎn)

Topoisomerase I

50 nM (IC 50 )

Protein Kinase C

160 μM (IC 50 )

體外研究

In the presence of human colon cancer cells labeled with 3 Hthymidine, edotecarin (0.6 μmol/L) increases the formation of DNA-protein complexes in a time-dependent manner.

體內(nèi)研究

Edotecarin produces an 83% increase in survival in mice bearing intracranial D-456MG glioma and shows a strong antimetastatic effect. Edotecarin results in tumor growth delays ranging from 10.45 days at the lowest dose (3 mg/kg) to 24.83 days at the highest (100 mg/kg). Combination treatment of edotecarin plus irinotecan improves antitumor activity in vivo compared with either agent alone.

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