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TP0427736 hydrochloride {[allProObj[0].p_purity_real_show]}

货号:A544247 Ambeed 开学季,买赠积分,赢豪礼

TP0427736 HCl is the HCl form of TP0427736 which is an inhibitor of ALK5 with IC50 of 2.72 nM and can reduce TGF-β induced growth.

TP0427736 hydrochloride 化学结构 CAS号:2459963-17-6
TP0427736 hydrochloride 化学结构
CAS号:2459963-17-6
TP0427736 hydrochloride 3D分子结构
CAS号:2459963-17-6
TP0427736 hydrochloride 化学结构 CAS号:2459963-17-6
TP0427736 hydrochloride 3D分子结构 CAS号:2459963-17-6
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TP0427736 hydrochloride 纯度/质量文件 产品仅供科研

货号:A544247 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 ALK 其他靶点 纯度
ASP3026 +

ALK, IC50: 3.5 nM

{[allProObj[0].p_purity_real_show]}
ALK-IN-1 ++++

ALK, IC50: 0.07 nM

{[allProObj[0].p_purity_real_show]}
Crizotinib ++++

ALK, IC50: 24 nM

ROS1, Ki: <0.025 nM

{[allProObj[0].p_purity_real_show]}
Entrectinib {[allProObj[0].p_purity_real_show]}
Brigatinib +++

ROS1, IC50: 1.9 nM

ALK, IC50: 0.37 nM

FLT3 {[allProObj[0].p_purity_real_show]}
NVP-TAE 684 +

ALK, IC50: 3 nM

{[allProObj[0].p_purity_real_show]}
Alectinib ++

ALK, IC50: 1.9 nM

ALK (F1174L), IC50: 3.5 nM

{[allProObj[0].p_purity_real_show]}
Ceritinib +++

ALK, IC50: 0.2 nM

Insulin Receptor,IGF-1R {[allProObj[0].p_purity_real_show]}
GSK1838705A +++

ALK, IC50: 0.5 nM

Insulin Receptor,IGF-1R {[allProObj[0].p_purity_real_show]}
AZD-3463 ++

ALK, Ki: 0.75 nM

IGF-1R {[allProObj[0].p_purity_real_show]}
Lorlatinib ++++

ALK (L1196M), Ki: 0.07 nM

ROS1, Ki: <0.07 nM

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Repotrectinib +

ALK(L1196M), IC50: 1.01 nM

ALK(G1202R), IC50: 1.26 nM

Src {[allProObj[0].p_purity_real_show]}
Belizatinib ++

ALK, IC50: 0.7 nM

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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

TP0427736 hydrochloride 生物活性

描述 The transforming growth factor-β (TGF-β) type I receptor kinase ALK5 (activin receptor-like kinase 5) is an attractive target for intervention in TGFβ signaling due to its druggability as well as its centrality and specificity in the pathway[1]. TP0427736 potently inhibited ALK5 activity, with an IC50 value of 2.72 nM. Its ability to inhibit ALK3 was quite low compared with ALK5, with an IC50 value of 836 nM.[2]. TP0427736 inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 in a concentration-dependent manner, with an IC50 value of 8.68 nM. TP0427736 rescues proliferation of outer root sheath cells suppressed by TGF-β[2]. The topical application of TP0427736 significantly decreased Smad2 phosphorylation in mouse skin, and its repeated application suppressed the shortening of average hair follicle length during the transition from the late anagen phase to the catagen phase[2]

TP0427736 hydrochloride 参考文献

[1]Ling LE, Lee WC. Tgf-beta type I receptor (Alk5) kinase inhibitors in oncology. Curr Pharm Biotechnol. 2011 Dec;12(12):2190-202. doi: 10.2174/138920111798808257. PMID: 21619541.

[2]Naruse T, Aoki M, Fujimoto N, Arase S, Oura H, Ueda Y, Ikeda A. Novel ALK5 inhibitor TP0427736 reduces TGF-β induced growth inhibition in human outer root sheath cells and elongates anagen phase in mouse hair follicles. Pharmacol Rep. 2017 Jun;69(3):485-491. doi: 10.1016/j.pharep.2017.01.024. Epub 2017 Jan 25. PMID: 28324846.

TP0427736 hydrochloride 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.99mL

0.60mL

0.30mL

14.93mL

2.99mL

1.49mL

29.86mL

5.97mL

2.99mL

TP0427736 hydrochloride 技术信息

CAS号2459963-17-6
分子式C14H11ClN4S2
分子量 334.847
别名
运输蓝冰
存储条件

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 2 mg/mL(5.97 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 3 mg/mL(8.96 mM),配合低频超声,并水浴加热至45℃助溶

动物实验配方
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