PHT-427|10mg|K1332-上海高创化学科技有限公司

SKU:K1332		M. Wt:409.61
Formula:C20H31N3O2S2		Solubility:No
Purity:>99%		Storage:2 years at -20 degrees centigrade
CAS No.:1191951-57-1, 1178893-77-0		Synonyms:N/A
Chemical NameN/A

Description	PHT-427
Targets	Akt	PDPK1
IC50	2.7 uM()	5.2 uM()
In vitro	PHT-427 can inhibit both Akt and PDPK1 with Ki values of 2.7 uM and 5.2 uM. PHT-427 itself (C-12 chain) bound with the highest affinity to the PH domains of both PDPK1 and Akt. PHT-427 inhibited Akt and PDKP1 signaling and their downstream targets in sensitive but not resistant cells and tumor xenografts. The PDPK1-independent phospho-Ser473-Akt was slightly increased by PHT-427, but completely inhibited in by wortmannin. Phospho-Ser657-protein kinase C (PKC) and total SGK1 are decreased by treatment with both PHT-427 and wortmannin. In the BxPC-3 cells which is sensitive to the antitumor activity of PHT-427, shows a decrease of both phospho-Ser473-Akt and phospho-Thr308-Akt.
In vivo	PHT-427 shows great antitumor activity. At doses of 125 to 250 mg/kg, PHT-427 gave up to an 80% inhibition of tumor growth in the most sensitive tumors.PHT-427 administered orally to mice with subcutaneous MCF-7 human breast cancer xenografts shows antitumor that was additive with that of paclitaxel. PHT-427 administered orally for 10 days to mice with orthotopic NCI-H441 NSC lung cancer xenografts increased the antitumor activity of continuous daily erlotinib which by itself had no antitumor activity in this model.
Clinical Trials	N/A
Features	N/A

Description

PHT-427

Targets

Akt

PDPK1

IC50

2.7 uM()

5.2 uM()

In vitro

PHT-427 can inhibit both Akt and PDPK1 with Ki values of 2.7 uM and 5.2 uM. PHT-427 itself (C-12 chain) bound with the highest affinity to the PH domains of both PDPK1 and Akt. PHT-427 inhibited Akt and PDKP1 signaling and their downstream targets in sensitive but not resistant cells and tumor xenografts. The PDPK1-independent phospho-Ser473-Akt was slightly increased by PHT-427, but completely inhibited in by wortmannin. Phospho-Ser657-protein kinase C (PKC) and total SGK1 are decreased by treatment with both PHT-427 and wortmannin. In the BxPC-3 cells which is sensitive to the antitumor activity of PHT-427, shows a decrease of both phospho-Ser473-Akt and phospho-Thr308-Akt.

In vivo

PHT-427 shows great antitumor activity. At doses of 125 to 250 mg/kg, PHT-427 gave up to an 80% inhibition of tumor growth in the most sensitive tumors.PHT-427 administered orally to mice with subcutaneous MCF-7 human breast cancer xenografts shows antitumor that was additive with that of paclitaxel. PHT-427 administered orally for 10 days to mice with orthotopic NCI-H441 NSC lung cancer xenografts increased the antitumor activity of continuous daily erlotinib which by itself had no antitumor activity in this model.

Clinical Trials

N/A

Features

N/A

工商信息

企业名称

上海高创化学科技有限公司

企业信息已认证

企业类型

信用代码

310228001353263

成立日期

2010-06-05

注册资本

经营范围

从事化学科技、计算机领域内技术开发、技术咨询、技术服务,从事生物科技领域内技术开发、技术咨询,化学试剂、化工原料及产品(除危险化学品、监控化学品、烟花爆竹、民用爆炸物品、易制毒化学品),实验室设备(除医疗器械),仪器仪表,Ⅰ类医疗器械,金属制品,电子产品,机电产品销售。【依法须经批准的项目,经相关部门批准后方可开展经营活动】

PHT-427由上海高创化学科技有限公司为您提供，货号K1332，规格：10mg，CAS号：1191951-57-1，如您想了解更多关于PHT-427价格、PHT-427结构式、批发、用途等信息，欢迎咨询。除供应PHT-427外，还可为您提供超级新生牛血清（无噬菌体低内毒素）、重组大鼠抵抗素(Rat Resistin)、豚鼠基质金属蛋白酶抑制因子1(TIMP-1)ELISA Kit等试剂，公司有专业的客户服务团队，是您值得信赖的合作伙伴，上海高创客户服务电话，售前、售后均可联系。