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AZ12601011 B
CAS No. 2748337-86-0
AZ12601011 B( —— )
Catalog No. M32795 CAS No. 2748337-86-0
AZ12601011 is an orally active, selective and potent TGFBR1 kinase inhibitor.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 152 | Get Quote |
|
| 5MG | 235 | Get Quote |
|
| 10MG | 376 | Get Quote |
|
| 25MG | 706 | Get Quote |
|
| 50MG | 1058 | Get Quote |
|
| 100MG | 1431 | Get Quote |
|
| 500MG | Get Quote | Get Quote |
|
| 1G | Get Quote | Get Quote |
|
Biological Information
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Product NameAZ12601011 B
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NoteResearch use only, not for human use.
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Brief DescriptionAZ12601011 is an orally active, selective and potent TGFBR1 kinase inhibitor.
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DescriptionAZ12601011 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 .
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In VitroAZ12601011 (0.01-10 μM; for 20 minutes) completely inhibits Phosphorylation of SMAD2 . AZ12601011 (0.01 μM-10 μM) inhibits the activity of ALK4, ALK7 and TGFBR1. AZ12601011 inhibits 4T1 cells growth in vitro (IC50=0.4μM) . Western Blot Analysis Cell Line:NIH3T3, HaCaT, C2C12, T47D cells Concentration:0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM Incubation Time:20 minutes Result:Completely inhibited Phosphorylation of SMAD2.
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In VivoAZ12601011 (50mg/kg; oral gavage; twice daily; for 25 days) inhibits tumour growth and metastasis in vivo. Animal Model:Female BALB/c mice at greater than 18g with tumour Dosage:50mg/kg Administration:Oral gavage; twice daily; for 25 days Result:Inhibited tumour growth and metastasis in vivo.
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Synonyms——
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PathwayAngiogenesis
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TargetALK
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RecptorALK | TGF-beta/Smad
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Research Area——
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Indication——
Chemical Information
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CAS Number2748337-86-0
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Formula Weight313.36
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Molecular FormulaC19H15N5
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 5 mg/mL (15.96 mM; Ultrasonic )
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SMILESN=1C=CC2=C(C1)C=CN2C3=NC(=NC4=C3CCC4)C5=NC=CC=C5
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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.?
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