CAS NO: | 1056901-62-2 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | AT13148 is an orally active and ATP-competitive, multi-AGC kinaseinhibitor withIC50s of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3,p70S6K,PKA, and ROCKI/II, respectively. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | AT13148 inhibits a panel of kinases at 10 μM, and the IC50values for p70S6K, PKA, ROCKI, and ROCKII are all less than 10 nM and those for AKT1, 2, and 3 are 38, 402, and 50 nM, respectively. For the related AGC kinases RSK1 and SGK3, the IC50values are 85 and 63 nM, respectively. In contrast, IC50values for the non-AGC kinases CHK2 and Aurora B are both greater than 800 nM. AT13148 potently inhibits proliferation with GI50values of 1.5 to 3.8 μM across a selected panel of cancer cell lines[1]. AT13148 treatment in gastric cancer cells dramatically suppresses activation of multiple AGC kinases, including Akt (at p-Thr-308), p70S6 kinase (p70S6K), glycogen synthase kinase 3β (GSK-3β) and p90 ribosomal S6 kinase (RSK)[2]. | ||||||||||||||||
体内研究 (In Vivo) | Oral drug administration of 5 mg/kg of AT13148 results in complete bioavailability. Clear inhibition of phosphorylation of the AKT substrates GSK3β, tuberin, and the p70S6K target S6RP are also observed in PTEN-deficient MES-SA human uterine tumor xenografts after treatment with 40 and 50 mg/kg p.o. of AT13148[1]. Oral gavage of AT13148 at well-tolerated doses significantly inhibits HGC27 xenograft tumor growth in nude mice. AGC activity is also dramatically decreased in AT13148-administrated HGC27 tumors[2]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 313.78 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C17H16ClN3O | ||||||||||||||||
CAS 号 | 1056901-62-2 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(159.35 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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