| Chemical Properties | Back Directory | [Boiling point ]
609.5±65.0 °C(Predicted) | [density ]
1.38±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
Solid | [pka]
2.00±0.10(Predicted) | [color ]
Light yellow to yellow | [InChI]
InChI=1S/C18H14N4OS/c1-11-2-8-14(9-3-11)21-18-22-17(20)16(24-18)15(23)13-6-4-12(10-19)5-7-13/h2-9H,20H2,1H3,(H,21,22) | [InChIKey]
CUDLEXBIVZPJBU-UHFFFAOYSA-N | [SMILES]
C(#N)C1=CC=C(C(C2SC(NC3=CC=C(C)C=C3)=NC=2N)=O)C=C1 |
| Hazard Information | Back Directory | [Description]
ABC1183 is a selective dual GSK3α/β and CKD9 inhibitor. | [Uses]
ABC1183 is an orally active selective dual GSK3 and CDK9 inhibitor. ABC1183 inhibits GSK3β, GSK3α and CDK9/cyclin T1 with the IC50 values of 657 nM, 327 nM and 321 nM, respectively. ABC1183 has anti-inflammatory and anti-tumor activities[1]. | [in vivo]
ABC1183 (oral gavage, 5 or 50 mg/kg) inhibits tumor proliferation through negative regulation of cell growth and pro-inflammatory signalling in male C57BL/6 mice[1].
| Animal Model: | Male C57BL/6 mice with melanoma B16[1] | | Dosage: | 5 mg/kg | | Administration: | Oral gavage; 5 times per week; 22 days | | Result: | Reduced tumor size and no observed toxicity.
Decreased the expression levels of GSK3 α /β, pSer21/9 and GS pSer641 but no change of total GS expression.
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| Animal Model: | Male C57BL/6 mice infected crohn’s disease[1] | | Dosage: | 50 mg/kg | | Administration: | Oral gavage; everyday; 3 days | | Result: | Reduced TNF-α by 65%, IL-6 by 30% and IL-1β by 45%. |
| Animal Model: | Male C57BL/6 mice with ulcerative colitis[1] | | Dosage: | 50 mg/kg | | Administration: | Oral gavage; once daily; 6 days | | Result: | Increased the expression of the anti-inflammatory factor IL-10, while decreasing the pro-inflammatory factor IL-6. |
| [IC 50]
CDK9- Cyclin T1: 321 nM (IC50); GSK-3α: 327 nM (IC50); GSK-3β: 657 nM (IC50) | [References]
[1] Randy S Schrecengost，et al. In Vitro and In Vivo Antitumor and Anti-Inflammatory Capabilities of the Novel GSK3 and CDK9 Inhibitor ABC1183. J Pharmacol Exp Ther. 2018 Apr;365(1):107-116. DOI:10.1124/jpet.117.245738 |
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| Company Name: |
DC Chemicals Gold
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| Tel: |
021-58447131 13564518121 |
| Website: |
www.chemicalbook.com/showsupplierproductslist927327/0_en.htm |
| Company Name: |
BOC Sciences
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| Tel: |
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| Website: |
https://www.bocsci.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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