CCT241736
Based on 1 Customer Validation
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).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.88%
- CAS No.: 1402709-93-6
- 화학식: C22H23Cl2N7
- 분자량:456.37
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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All Aurora Kinase Isoforms
More
Biological Activity
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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) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | GI50 |
0.3 nM
Compound: 27e
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Growth inhibition of human HCT116 cells
Growth inhibition of human HCT116 cells
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[PMID: 23043539] |
| HeLa | IC50 |
0.03 μM
Compound: 27e
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Inhibition of Aurora A kinase autophosphorylation at T288 in human HeLa cells
Inhibition of Aurora A kinase autophosphorylation at T288 in human HeLa cells
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[PMID: 23043539] |
| HeLa | IC50 |
0.148 μM
Compound: 27e
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Inhibition of Aurora B kinase-mediated Histone H3 phosphorylation at S10 in human HeLa cells
Inhibition of Aurora B kinase-mediated Histone H3 phosphorylation at S10 in human HeLa cells
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[PMID: 23043539] |
| MOLM-13 | GI50 |
0.104 nM
Compound: 27e
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Growth inhibition of human MOLM13 cells
Growth inhibition of human MOLM13 cells
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[PMID: 23043539] |
| MOLM-13 | GI50 |
100 nM
Compound: 23; CCT241736
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Antiproliferative activity against human MOLM-13 cells incubated for 72 hrs by MTS assay
Antiproliferative activity against human MOLM-13 cells incubated for 72 hrs by MTS assay
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[PMID: 33719439] |
| MOLM-13 | GI50 |
180 nM
Compound: 23; CCT241736
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Antiproliferative activity against drug resistant human MOLM-13 cells incubated for 72 hrs by MTS assay
Antiproliferative activity against drug resistant human MOLM-13 cells incubated for 72 hrs by MTS assay
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[PMID: 33719439] |
| SW-620 | GI50 |
0.283 μM
Compound: 27e
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Growth inhibition of human SW620 cells after 72 hrs by MTT assay
Growth inhibition of human SW620 cells after 72 hrs by MTT assay
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[PMID: 23043539] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1402709-93-6
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Appearance Solid
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분자량 456.37
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화학식 C22H23Cl2N7
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Color White to off-white
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SMILES
CC1=NN(C)C=C1C2=NC3=C(N4CCN(CC5=CC=C(Cl)C=C5)CC4)C(Cl)=CN=C3N2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
용액&용해도
DMSO : 12.5 mg/mL (27.39 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.48 mM); Suspended solution; Need ultrasonic and warming
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.48 mM); Suspended solution; Need ultrasonic and warming
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1912 mL | 10.9560 mL | 21.9120 mL | 54.7801 mL |
| 5 mM | 0.4382 mL | 2.1912 mL | 4.3824 mL | 10.9560 mL | |
| 10 mM | 0.2191 mL | 1.0956 mL | 2.1912 mL | 5.4780 mL | |
| 15 mM | 0.1461 mL | 0.7304 mL | 1.4608 mL | 3.6520 mL | |
| 20 mM | 0.1096 mL | 0.5478 mL | 1.0956 mL | 2.7390 mL | |
| 25 mM | 0.0876 mL | 0.4382 mL | 0.8765 mL | 2.1912 mL |
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