PHT-427|10mg|K1332-上海高创化学科技有限公司

PHT-427

参考价：¥793

供货周期：

一周

品牌：

规格：

10mg

货号：

K1332

CAS号：

1191951-57-1

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