LY2784544|2mg|K1311-上海高创化学科技有限公司

LY2784544

参考价：¥1298

供货周期：

一周

品牌：

规格：

2mg

货号：

K1311

CAS号：

1229236-86-5

SKU:K1311		M. Wt:469.94
Formula:C23H25ClFN7O		Solubility:No
Purity:>99%		Storage:2 years at -20 degrees centigrade
CAS No.:1229236-86-5		Synonyms:N/A
Chemical NameN/A

Description	LY2784544
Targets	JAK2 V617F
IC50	55 nM
In vitro	LY2784544 potently inhibited the JAK2 V617F-STAT5 signaling with IC50 of 55 nM, but the IC50 for inhibiting wild type JAK2 is 2.26 uM. LY2784544 selectively inhibit the JAK2 V617F-driven cell proliferation with IC50 of 68 nM.In Ba/F3 cell model, LY2784544 can inhibit JAK2 V617F signaling and induce apoptosis with EC50 of 113 nM.
In vivo	In vivo, LY2784544 effectively inhibits STAT5 phosphorylation in Ba/F3-JAK2 V617F-GFP ascites tumor cells with a Threshold Effective Dose 50 (TED50) of 12.7 mg/kg. LY2784544 also significantly duced Ba/F3-JAK2 V617F-GFP tumor burden in the JAK2 V617F-induced MPN model with a TED50 of 13.7 mg/kg after oral treatment (BID) for 14 days.LY2784544 selectively reduced Ba/F3-JAK2 V617F-GFP tumor cells with no effect on CD71/Ter119 positive erythroid progenitors in spleens of SCID mice after oral treatment (BID) for seven days.
Clinical Trials	N/A
Features	N/A

Description

LY2784544

Targets

JAK2 V617F

IC50

55 nM

In vitro

LY2784544 potently inhibited the JAK2 V617F-STAT5 signaling with IC50 of 55 nM, but the IC50 for inhibiting wild type JAK2 is 2.26 uM. LY2784544 selectively inhibit the JAK2 V617F-driven cell proliferation with IC50 of 68 nM.In Ba/F3 cell model, LY2784544 can inhibit JAK2 V617F signaling and induce apoptosis with EC50 of 113 nM.

In vivo

In vivo, LY2784544 effectively inhibits STAT5 phosphorylation in Ba/F3-JAK2 V617F-GFP ascites tumor cells with a Threshold Effective Dose 50 (TED50) of 12.7 mg/kg. LY2784544 also significantly duced Ba/F3-JAK2 V617F-GFP tumor burden in the JAK2 V617F-induced MPN model with a TED50 of 13.7 mg/kg after oral treatment (BID) for 14 days.LY2784544 selectively reduced Ba/F3-JAK2 V617F-GFP tumor cells with no effect on CD71/Ter119 positive erythroid progenitors in spleens of SCID mice after oral treatment (BID) for seven days.

Clinical Trials

N/A

Features

N/A