产品名称 AZD 5363 from LIFESPAN BIOSCIENCES INC.
产品货号 LS-H6706
产品价格 现货询价,电话:010-67529703
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产品品牌 LIFESPAN BIOSCIENCES INC.
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Product NameAZD 5363
DescriptionPurity >98%. Akt functions as a key component in multiple signaling pathways including those related to cell proliferation, metabolism, and survival as well as angiogenesis. AZD 5363 is a pyrrolopyrimidine-derived compound that inhibits Akt by competitively binding to the kinase domain, preventing substrate phosphorylation by Akt. It inhibits Akt1, 2, and 3 with IC50 values of 3, 7, and 7 nM, respectively and also inhibits P70S6K and PKA with similar potency (IC50 s = 6 and 7 nM, respectively). Furthermore, AZD 5363 shows >75% inhibition at 1 µM against ROCK-II, MKK1, MSK1, MSK2, PKCGamma, PKGAlpha, PKGBeta, PRKX, RSK2, and RSK3. At 3 µM or less, AZD 5363 has been reported to inhibit the proliferation of 41 out of 182 solid and hematologic tumor cell lines, demonstrating the greatest sensitivity towards breast cancer derived-cells or those with PIK3CA and/or PTEN mutations. Oral dosing to nude mice bearing BT474c xenografts resulted in antitumor activity, including the reduction of the phosphorylation of PRAS40, GSK3Beta, and S6 at an EC50 value of ~ 0.1 µM.
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Other Names4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinecarboxamide
Gene, Accession, CAS #CAS: 1143532-39-1
Catalog #LS-H6706
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Order / More InfoAZD 5363 from LIFESPAN BIOSCIENCES INC.
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