| Chemical Properties | Back Directory | [Boiling point ]
416.5±45.0 °C(predicted) | [density ]
1.38±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
Solid | [pka]
6.71±0.30(predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth [1]. | [Biological Activity]
AZ12601011 is an orally activesubtype-selective TGF-β type I receptors active site inhibitor (active-site affinity: ALK4/5/6 Kd = 2.6/2.9/42 nMALK1/2/3 Kd = 40/15/40 μM) th at prevents ALK4/5/7-mediated Smad2but not ALK1/2/3/6-mediated Smad1phosphorylation (10 μM; NIH3T3 expressing respective constitutively active receptors). AZ12601011 inhibits 4T1 murine mammary carcinoma growth in cultures (IC50 = 400 nM) and in vivo (50 mg/kg bid. po. mice). AZ12601011 also causes heart valve lesions and physeal dysplasia in rats (150 mg/kg/day po. for 7 days)consistent with a critical role of ALK5 in maintaining the integrity of heart valve and physis. | [in vivo]
AZ12601011 (50mg/kg; oral gavage; twice daily; for 25 days) inhibits tumour growth and metastasis in vivo[1].
| Animal Model: | Female BALB/c mice at greater than 18g with tumour[1] | | Dosage: | 50mg/kg | | Administration: | Oral gavage; twice daily; for 25 days | | Result: | Inhibited tumour growth and metastasis in vivo.
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| [IC 50]
ALK4; ALK7 | [References]
[1] Spender LC, et al. Preclinical Evaluation of AZ12601011 and AZ12799734, Inhibitors of Transforming Growth Factor βSuperfamily Type 1 Receptors. Mol Pharmacol. 2019 Feb;95(2):222-234. DOI:10.1124/mol.118.112946 |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|