| Identification | Back Directory | [Name]
A-770041 | [CAS]
869748-10-7 | [Synonyms]
A-770041
N-[4-[1-[4-(4-acetylpiperazin-1-yl)cyclohexyl]-4-aminopyrazolo[3,4-d]pyrimidin-3-yl]-2-methoxyphenyl]-1-methylindole-2-carboxamide
N-[4-[1-[trans-4-(4-Acetyl-1-piperazinyl)cyclohexyl]-4-amino-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-2-methoxyphenyl]-1-methyl-1H-indole-2-carboxamide
1H-Indole-2-carboxamide, N-[4-[1-[trans-4-(4-acetyl-1-piperazinyl)cyclohexyl]-4-amino-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-2-methoxyphenyl]-1-methyl-
N-(4-(1-((1r,4r)-4-(4-acetylpiperazin-1-yl)cyclohexyl)-4-amino-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-methoxyphenyl)-1-methyl-1H-indole-2-carboxamide | [Molecular Formula]
C34H39N9O3 | [MDL Number]
MFCD24873124 | [MOL File]
869748-10-7.mol | [Molecular Weight]
621.73 |
| Chemical Properties | Back Directory | [Boiling point ]
812.6±65.0 °C(Predicted) | [density ]
1.42±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
0.1 M HCl: 20 mg/ml; DMSO: 20 mg/ml; Ethanol: 2 mg/ml | [form ]
Powder | [pka]
13.21±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
A-770041 is a selective and orally active Src-family Lck inhibitor. A-770041 inhibits Lck with an IC50 value of 147 nM with the presence of 1 mM ATP. A-770041 shows 300-fold selective to Lck over Fyn, the other Src family kinase involved in T-cell signaling. A-770041 can be used for the research of acute rejection[1][2]. | [Definition]
ChEBI: N-[4-[1-[4-(4-acetyl-1-piperazinyl)cyclohexyl]-4-amino-3-pyrazolo[3,4-d]pyrimidinyl]-2-methoxyphenyl]-1-methyl-2-indolecarboxamide is an aromatic amide. | [in vivo]
A-770041 (2.5 mg/kg; i.g. once) inhibits concanavalin A-induced IL-2 in vivo[1].
A-770041 (2.5-20 mg/kg/day; for 14 days) dose-dependently increases the survival rate with doses of 5 and 10 mg/kg/day, and survives 100% of transplanted grafts until 14 days with doses of 10 and 20 mg/kg/day[1]. | Animal Model: | Male Lewis rats[1] | | Dosage: | 2.5 mg/kg | | Administration: | Intragastric administration; 2.5 mg/kg once | | Result: | Showed an inhibition of concanavalin A-induced IL-2 with an in vivo EC50 value of 78 nM. |
| [References]
[1] Stachlewitz RF, et al.A-770041, a novel and selective small-molecule inhibitor of Lck, prevents heart allograft rejection.J Pharmacol Exp Ther. 2005 Oct;315(1):36-41. DOI:10.1124/jpet.105.089169
[2] Andrew Burchat, et al. Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection Bioorganic & Medicinal Chemistry Letters Volume 16, Issue 1, 1 January 2006, Pages 118-122 DOI:10.1016/j.bmcl.2005.09.039 |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
|