6-bromo-7-(4-((5-methylisoxazol-3-yl)methyl)piperazin-1-yl)-2-(4-(4-methylpiperazin-1-yl)phenyl)-3H-imidazo[4,5-b]pyridine
CCT137690
CAS: 1095382-05-0
Molecular Formula: C26H31BrN8O
6-bromo-7-(4-((5-methylisoxazol-3-yl)methyl)piperazin-1-yl)-2-(4-(4-methylpiperazin-1-yl)phenyl)-3H-imidazo[4,5-b]pyridine - Names and Identifiers
6-bromo-7-(4-((5-methylisoxazol-3-yl)methyl)piperazin-1-yl)-2-(4-(4-methylpiperazin-1-yl)phenyl)-3H-imidazo[4,5-b]pyridine - Physico-chemical Properties
| Molecular Formula | C26H31BrN8O |
| Molar Mass | 551.48 |
| Density | 1.424 |
| Storage Condition | 2-8℃ |
| Use | CCT137690 is a highly selective Aurora A, Aurora B and Aurora C inhibitor with IC50 of 15 nM, 25 nM and 19 nM, respectively, with little effect on hERG ion channels. |
| In vitro study | CCT137690 has anti-proliferative activity on a variety of human tumor cell lines, including SW620 colon cancer cells and A2780 ovarian cancer cells, with GI50 of 0.3 and 0.14 μm, respectively. In addition, CCT137690 also inhibited the phosphorylation of histone H3. CCT137690 inhibits the major cytochrome P450 subtypes (CYP1A2,CYP2A6,CYP2C9,CYP2C19,CYP2D6, CYP3A4) with IC50 values greater than 10 μm. However, CCT137690 is a modest inhibitor of hERG ion channels with an IC50 of 3.0 μm. CCT137690 is effective in inhibiting the growth of tumor cell lines of different human organs with GI50 values ranging from 0.005 to 0.47 μm. CCT137690 completely inhibited Aurora A autophosphorylation at the T288 site, and also inhibited histone H3 phosphorylation at 0.5 μm. CCT137690 acts on HCT116 cells to induce polyploidy, mitotic aberration, and apoptosis. CCT137690 acts on the KELLY neuroblastoma cell line, reducing MYCN levels, and GSK3β phosphorylation. CCT137690 inhibits FLT3 autophosphorylation, and phosphorylation of downstream targets STAT5 and p44/42 MAPK(Erk1/2). CCT137690 acts on FLT3-ITD positive AML, inhibits Aurora and FLT3 kinase, induces apoptosis, and causes the cell cycle to appear to accumulate at the G2/M phase. |
| In vivo study | In vivo, oral treatment of CCT137690 inhibited the growth of SW620 colon cancer xenografts without significant cytotoxicity. Overexpression of MYCN protein in transgenic mouse neuroblastoma model, and easy to spontaneous formation of neuroblastoma, CCT137690 significantly inhibited tumor growth. In addition, CCT137690 was effective in inhibiting subcutaneous MOLM-13 of transplanted tumors, and there was no significant toxicity and no decrease in body weight. |
6-bromo-7-(4-((5-methylisoxazol-3-yl)methyl)piperazin-1-yl)-2-(4-(4-methylpiperazin-1-yl)phenyl)-3H-imidazo[4,5-b]pyridine - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.813 ml | 9.067 ml | 18.133 ml |
| 5 mM | 0.363 ml | 1.813 ml | 3.627 ml |
| 10 mM | 0.181 ml | 0.907 ml | 1.813 ml |
| 5 mM | 0.036 ml | 0.181 ml | 0.363 ml |
Last Update：2024-01-02 23:10:35
6-bromo-7-(4-((5-methylisoxazol-3-yl)methyl)piperazin-1-yl)-2-(4-(4-methylpiperazin-1-yl)phenyl)-3H-imidazo[4,5-b]pyridine - Reference Information
| biological activity | CCT137690 is a highly selective Aurora A, Aurora B and Aurora C inhibitor with IC50 of 15 nM, 25 nM and 19 nM respectively, which has little effect on hERG ion channels. |
| in vitro study | CCT137690 has antiproliferative activity on a variety of human tumor cell lines, including SW620 colon cancer cells and A2780 ovarian cancer cells, with GI50 of 0.3 and 0.14 μM respectively. In addition, CCT137690 also inhibited the phosphorylation of histone H3. CCT137690 inhibited the main cytochrome P450 subtypes (CYP1A2,CYP2A6,CYP2C9,CYP2C19,CYP2D6, CYP3A4), and the IC50 value was 10 μM larger. However, CCT137690 is a moderate inhibitor of hERG ion channels with an IC50 of 3.0 μM. CCT137690 effectively inhibit the growth of tumor cell lines in different human organs, GI50 values are 0.005 to 0.47 μM. CCT137690 completely inhibited Aurora A autophosphorylation at T288 site, and also inhibited histone H3 phosphorylation at 0.5 μM. CCT137690 acts on HCT116 cells to induce polyploidy, mitotic distortion and apoptosis. CCT137690 acts on KELLY neuroblastoma cell line to reduce MYCN level and GSK3β phosphorylation. CCT137690 inhibits FLT3 autophosphorylation and phosphorylation of downstream targets STAT5 and p44/42 MAPK(Erk1/2). CCT137690 acts on FLT3-ITD positive AML, inhibits Aurora and FLT3 kinase, induces apoptosis, and leads to cell cycle accumulation in G2/M phase. |
| in vivo study | in vivo, oral treatment of CCT137690 inhibits the growth of SW620 colon cancer transplanted tumor without obvious cytotoxicity. MYCN protein is overexpressed in transgenic mouse neuroblastoma model, and it is easy to spontaneously form neuroblastoma, which CCT137690 significantly inhibit tumor growth. In addition, the CCT137690 effectively inhibited subcutaneous MOLM-13 transplanted tumor without obvious toxicity and weight loss. |
| Features | CCT137690 are inhibitors of oral effectiveness and have reasonable pharmacokinetic parameters. |
| target | Aurora A 15 nM (IC 50 ) Aurora B 25 nM (IC 50 ) Aurora C 19 nM (IC 50 ) |
Last Update：2024-04-09 21:50:46
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Product Name: CCT137690 Visit Supplier Webpage Request for quotation
CAS: 1095382-05-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1095382-05-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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