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28755-03-5

中文名稱 2-氯-1-(1H-吲哚-3-基)-乙酮
英文名稱 Ethanone, 2-chloro-1-(3-indolyl)-
CAS 28755-03-5
分子式 C10H8ClNO
分子量 193.63
MOL 文件 28755-03-5.mol
28755-03-5 結(jié)構(gòu)式 28755-03-5 結(jié)構(gòu)式

基本信息

中文別名
3-氯乙?;胚?BR>2-氯-1-(3-吲哚基)-乙酮
乙酮,2-氯-1H-吲哚-1-基-
乙酮,2-氯-1-(3-吲哚基)-
2-氯-1-(1H-吲哚-3-基)-乙酮
乙酮,2-氯-1-(1H-吲哚-3-基)-
英文別名
3CAI
3CAI >=95% (HPLC)
3-chloroacetylindole
Akt Inhibitor XIX, 3CAI
Chloromethyl indol-3-yl ketone
3-(Chloroacetyl)-1H-indole 95%
2-Chloro-1-(3-Indolyl)-Ethanone
Ethanone, 2-chloro-1-(3-indolyl)-
Ethanone, 2-chloro-1H-indol-1-yl-
Ethanone, 2-chloro-1-(1H-indol-3-yl)-

物理化學(xué)性質(zhì)

熔點(diǎn)212-214 °C(Solv: ethyl ether (60-29-7))
沸點(diǎn)379.1±17.0 °C(Predicted)
密度1.337±0.06 g/cm3(Predicted)
儲(chǔ)存條件Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
溶解度DMSO:可溶,5mg/mL,澄清
酸度系數(shù)(pKa)15.08±0.30(Predicted)
形態(tài)粉末
顏色黃色到棕色

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H319
防范說(shuō)明P305+P351+P338
危險(xiǎn)品標(biāo)志Xn
危險(xiǎn)類別碼22-36
安全說(shuō)明26
WGK Germany3
海關(guān)編碼2933998090
2-氯-1-(1H-吲哚-3-基)-乙酮價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/08HY-166662-氯-1-(1H-吲哚-3-基)-乙酮
3CAI
28755-03-55mg580元
2024/11/08HY-166662-氯-1-(1H-吲哚-3-基)-乙酮
3CAI
28755-03-510mM * 1mLin DMSO638元
2024/11/08HY-166662-氯-1-(1H-吲哚-3-基)-乙酮
3CAI
28755-03-510mg859元

常見(jiàn)問(wèn)題列表

生物活性
3CAI 是一種有效的特異性 AKT1 和 AKT2 抑制劑。
靶點(diǎn)

Akt1

Akt2

體外研究

3CAI is a potential inhibitor of AKT. Based on these screening data, the effect of 3CAI on the kinase activities of AKT1, MEK1, JNK1, ERK1 and TOPK is tested using in vitro kinase assays. The results show that 3CAI (1 μM) suppresses only AKT1 kinase activity and the other kinases tested are not affected by 3CAI. 3CAI is a much more potent AKT1 inhibitor than PI3K (60% inhibition at 1 vs 10 μM, respectively). 3CAI substantially suppresses AKT1 activity as well as AKT2 activity in a dose dependent manner. 3CAI inhibits down-stream targets of AKT and induces apoptosis. AKT-mediated phosphorlyation site of mTOR (Ser2448) and GSK3β (Ser9) are substantially decreased by 3CAI in a time-dependent manner. Furthermore, pro-apoptotic marker proteins p53 and p21 are also upregulated by 3CAI after 12 or 24 h of treatment. HCT116 and HT29 colon cancer cells are seeded on 6 cm dishes in 1% FBS/McCoy's 5A (HCT116) with 3CAI (4 μM), I3C or the AKT inhibitor and then incubated for 4 days. Results show that the number of apoptotic cells is significantly increased by 3CAI in HCT116 and HT29 colon cancer cells compared with untreated control cells.

體內(nèi)研究

To examine the antitumor activity of 3CAI in vivo, HCT116 cancer cells are injected into the right flank of individual athymic nude mice. Mice are orally administered 3CAI at 20 or 30 mg/kg, I3C at 100 mg/kg, or vehicle 5 times a week for 21 days. Treatment of mice with 30 mg/kg of 3CAI significantly suppresses HCT116 tumor growth by 50% relative to the vehicle-treated group (p<0.05). Remarkably, mice seem to tolerate treatment with these doses of 3CAI without overt signs of toxicity or significant loss of body weight compared with vehicle-treated group. Expression of these AKT-target proteins is strongly suppressed by 30 mg/kg of 3CAI in tumor tissues.

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