AZ12601011( AZ-12601011 | AZ 12601011 )

Catalog No. M16993 CAS No. ——

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

AZ12601011
Note

Research use only, not for human use.
Brief Description

AZ12601011 (AZ-12601011) is a potent, selective inhibitor of ALK4, ALK7 and TGFBR1 (Kd=2.9 nM).
Description

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.
In Vitro

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In Vivo

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Synonyms

AZ-12601011 | AZ 12601011
Pathway

TGF-beta/Smad
Target

TGFBR
Recptor

TGFBR
Research Area

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Indication

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CAS Number

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Formula Weight

313.364
Molecular Formula

C19H15N5
Purity

>98% (HPLC)
Solubility

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SMILES

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Chemical Name

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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