AZ12601011 ( AZ-12601011 | AZ 12601011 )

产品货号. M16993 CAS No. ——

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

AZ12601011
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

AZ12601011 (AZ-12601011) 是一种有效的选择性 ALK4、ALK7 和 TGFBR1 抑制剂 (Kd=2.9 nM)。
产品描述

AZ12601011 (AZ-12601011) is a potent, selective inhibitor of ALK4, ALK7 and TGFBR1 (Kd=2.9 nM), inhibits TGFβ-induced reporter activity with IC50 of 18 nM; inhibits TGFBR1 kinase activity (competition binding) with Kd of 2.9 nM, shows some inhibitory activity against the related receptors ALK4 and BMPR1B, but shows only weakly activity against ALK1, ALK2 and BMPR1A in in vitro kinase assays; AZ12601011 is a more effective inhibitor of TGFβ-induced reporter activity than SB-431542 (IC50=84nM) and LY2157299 (galunisertib) (IC50=380nM), inhibits phosphorylation of SMAD2 via the type 1 receptors ALK4, TGFBR1 and ALK7; AZ12601011 is highly effective at inhibiting basal and TGFβ-induced migration of HaCaT keratinocytes, inhibits tumour growth and metastasis to the lungs in a 4T1 syngeneic orthotopic mammary tumour model.
体外实验

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体内实验

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同义词

AZ-12601011 | AZ 12601011
通路

TGF-beta/Smad
靶点

TGFBR
受体

TGFBR
研究领域

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适应症

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CAS Number

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分子量

313.364
分子式

C19H15N5
纯度

>98% (HPLC)
溶解度

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SMILES

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化学全称

2-(pyridin-2-yl)-4-(1H-pyrrolo[3,2-c]pyridin-1-yl)-6,7-dihydro-5H-cyclopenta[d]pyrimidine

1. Spender LC, et al. Mol Pharmacol. 2018 Nov 20. pii: mol.118.112946. doi: 10.1124/mol.118.112946.

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