CCT241736 |
Catalog No.GC19092
One-Click Copy Product Info
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CCT241736 est un inhibiteur double FLT3 et Aurora kinase puissant et biodisponible par voie orale, qui inhibe les kinases Aurora (Aurora-A Kd, 7,5 nM, IC50, 38 nM ; Aurora-B Kd, 48 nM), la kinase FLT3 (Kd, 6,2 nM), et des mutants FLT3 comprenant FLT3-ITD (Kd, 38 nM) et FLT3(D835Y) (Kd, 14 nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1402709-93-6
Sample solution is provided at 25 µL, 10mM.
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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).
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 uM), the human FLT3-ITD positive AML cell lines MOLM-13 (GI50, 0.104 uM) and MV4-11 (GI50, 0.291 uM). CCT241736 also inhibits both the autophosphorylation of Aurora-A at T288 (a biomarker for Aurora-A inhibition: IC50, 0.030 uM) and histone H3 phosphorylation at S10 (a biomarker for Aurora-B inhibition: IC50, 0.148 uM), 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].
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].
References:
[1]. Bavetsias V, et al. Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia. J Med Chem. 2012 Oct 25;55(20):8721-34.
Animal experiment: | 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: [1]. Bavetsias V, et al. Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia. J Med Chem. 2012 Oct 25;55(20):8721-34. | |
| Cas No. | 1402709-93-6 | SDF | |
| Canonical SMILES | CC1=NN(C)C=C1C2=NC3=C(N4CCN(CC5=CC=C(Cl)C=C5)CC4)C(Cl)=CN=C3N2 | ||
| Formula | C22H23Cl2N7 | M.Wt | 456.37 |
| Solubility | DMSO : 75 mg/mL (164.34 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1912 mL | 10.956 mL | 21.912 mL |
| 5 mM | 438.2 μL | 2.1912 mL | 4.3824 mL |
| 10 mM | 219.1 μL | 1.0956 mL | 2.1912 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)