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首页-小分子抑制剂&激动剂-TGF-beta/Smad-TGF beta Receptor (TGFBR)-AZ12601011
AZ12601011

Chemical Structure : AZ12601011

CAS No.: 2748337-86-0

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AZ12601011 (AZ-12601011;AZ 12601011)

货号: PC-35811Not For Human Use, Lab Use Only.

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.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.
    AZ12601011 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.
    AZ12601011 inhibits tumour growth and metastasis to the lungs in a 4T1 syngeneic orthotopic mammary tumour model.

    物理化学性质&存储条件

    分子量 313.364
    分子式 C19H15N5
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

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

    参考文献

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

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