CCT241736
Modify Date: 2024-01-04 10:14:42
CCT241736 structure
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Common Name | CCT241736 | ||
|---|---|---|---|---|
| CAS Number | 1402709-93-6 | Molecular Weight | 456.371 | |
| Density | 1.5±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C22H23Cl2N7 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of CCT241736CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A Kd, 7.5 nM, IC50, 38 nM; Aurora-B Kd, 48 nM), FLT3 kinase (Kd, 6.2 nM), and FLT3 mutants including FLT3-ITD (Kd, 38 nM) and FLT3(D835Y) (Kd, 14 nM). |
| Name | CCT241736 |
|---|---|
| Synonym | More Synonyms |
| Description | CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A Kd, 7.5 nM, IC50, 38 nM; Aurora-B Kd, 48 nM), FLT3 kinase (Kd, 6.2 nM), and FLT3 mutants including FLT3-ITD (Kd, 38 nM) and FLT3(D835Y) (Kd, 14 nM). |
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| Related Catalog | |
| Target |
Aurora-A:38 nM (IC50) Aurora-A:7.5 nM (Kd) Aurora-B:48 nM (Kd) FLT3(K663Q):5.1 nM (Kd) FLT3:6.2 nM (Kd) FLT3(D835H):11 nM (Kd) FLT3(D835Y):14 nM (Kd) FLT3(N841I):16 nM (Kd) FLT3-ITD:38 nM (Kd) FLT3(R834Q):110 nM (Kd) |
| In Vitro | CCT241736 (Compound 27e) is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A Kd, 7.5 nM, IC50, 38 nM, Aurora-B Kd, 48 nM), FLT3 kinase (Kd, 6.2 nM), and FLT3 mutants including FLT3-ITD (Kd, 38 nM) and FLT3(D835Y) (Kd, 14 nM). CCT241736 exhibits antiproliferative activity in a range of human tumor cell lines, such as HCT116 human colon carcinoma (GI50, 0.300 μM), the human FLT3-ITD positive AML cell lines MOLM-13 (GI50, 0.104 μM) and MV4-11 (GI50, 0.291 μM). CCT241736 also inhibits both the autophosphorylation of Aurora-A at T288 (a biomarker for Aurora-A inhibition: IC50, 0.030 μM) and histone H3 phosphorylation at S10 (a biomarker for Aurora-B inhibition: IC50, 0.148 μM), consistent with potent cellular activity versus both Aurora-A and -B. CCT241736 suppresses Aurora-A in MOLM-13 cells with concomitant inhibition of FLT3 signaling[1]. |
| In Vivo | CCT241736 (50, 100 mg/kg, b.i.d, p.o.) dose-dependently suppresses the growth of MV4-11 human tumor xenografts, and completely abolishes the tumors at 100 mg/kg via p.o. administration twice a day[1]. |
| Animal Admin | Mice[1] Female adult CrTacNCr-Fox1(nu) athymic mice are implanted subcutaneously with 107 FLT3-ITD-positive MV4-11 human leukemia cells. When the tumor xenografts are well-established (10 days after implantation, mean tumor volumes of at least 100 mm3), animals are treated with either vehicle (10% DMSO, 20% PEG 400, 5% Tween 80 and 65% water) or CCT241736 administered orally at two doses, 50 and 100 mg/kg (n = 5 per group). Dosing is twice daily for 7 days, and once daily for a further 4 days[1]. |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Molecular Formula | C22H23Cl2N7 |
| Molecular Weight | 456.371 |
| Exact Mass | 455.139191 |
| LogP | 4.55 |
| Index of Refraction | 1.727 |
| Storage condition | 2-8℃ |
| 6-Chloro-7-[4-(4-chlorobenzyl)-1-piperazinyl]-2-(1,3-dimethyl-1H-pyrazol-4-yl)-1H-imidazo[4,5-b]pyridine |
| 3H-Imidazo[4,5-b]pyridine, 6-chloro-7-[4-[(4-chlorophenyl)methyl]-1-piperazinyl]-2-(1,3-dimethyl-1H-pyrazol-4-yl)- |