產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO)5mg
CAS	552325-16-3
別名	A 443654; A443654
化學(xué)名	(2S)-1-(1H-indol-3-yl)-3-[5-(3-methyl-2H-indazol-5-yl)pyridin-3-yl]oxypropan-2-amine
分子式	C24H23N5O
分子量	397.48
溶解度	≥ 19.85 mg/mL in DMSO, ≥ 44.3 mg/mL in EtOH
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

A-443654 is a potent and selective inhibitor of Akt with Ki value of 160 pM [1].

The Akt kinases play important roles in cellular signal transduction and take participate in the regulation of cell transformation and tumor progression. The activities of them are usually elevated in human malignancies. A-443654 is a pan inhibitor of Akt1, 2 and 3. It binds to the ATP-binding site of Akt and inhibits the kinase activity reversibly. A-443654 shows selectivity against Akt. The inhibition ability of it for Akt is much higher than that for other kinases. It is found that A-443654 can suppress the phosphorylation of the downstream proteins of Akt while increased the Ser473 and Thr308 phosphorylation of Akt [1].

In murine FL5.12 cells stably transfected with human Akt1, 2 or 3, A-443654 inhibited the phosphorylation of GSK3 dose-dependently. A-443654 at a concentration of 0.6 μM inhibited Akt and induced G2/M accumulation in H1299 cells. In MiaPaCa-2 cells, treatment of A-443654 for 48 h resulted in a suppression of tumor proliferation with EC50 value of 100 nM. In chronic lymphocytic leukemia cells, A-443654 also inhibited the activity of Akt and induced apoptosis with EC50 value of 0.63 μM .Besides that, A-443654 was found to cause decreased phosphorylation of GSK3, FOXO3, TSC2 and mTOR in MiaPaCa-2 cells. It is also reported that A-443654 was effective in blocking the phosphorylation of 4EBP-1 and S6 protein in both T47D and LNCaP cells [1, 2, 3 and 4].

A-443654 is not oral available. In mice model with human MiaPaCa-2 pancreatic cell xenograft, the administration of A-443654 at a dose of 7.5mg/kg/d significantly inhibited tumor growth. A-443654 also inhibited tumor growth in 3T3 murine fibroblast model expressing active Akt. When using the combination of A-443654 and rapamycin in mice model with MiaPaCa-2 pancreatic cancer xenograft, the administration showed more efficacy than each monotherapy [1].

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請穿好實(shí)驗(yàn)服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術(shù)有限公司

在線咨詢

留言注意事項(xiàng)：

1.遵守中華人民共和國有關(guān)法律、法規(guī)，尊重網(wǎng)上道德，承擔(dān)一切因您的行為而直接或間接引起的法律責(zé)任。

2.請您真實(shí)的反映產(chǎn)品的情況,不要捏造、誣蔑、造謠。如對產(chǎn)品有任何疑問,也可以留言咨詢。

3.未經(jīng)本站同意，任何人不得利用本留言簿發(fā)布個(gè)人或團(tuán)體的具有廣告性質(zhì)的信息或類似言論。

您感興趣的產(chǎn)品*
您的單位*
聯(lián)系人*
聯(lián)系電話*
詳細(xì)地址*
常用郵箱*
請輸入您對我們的意見或建議*
驗(yàn)證碼*