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| 50mg |
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| 250mg |
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CB-6644 is a novel, potent, and selective inhibitor of RUVBL1/2 complex with anticancer activity, blocking the ATPase activity of RUVBL1/2 with an IC50 of 15 nM.
| ln Vitro |
In Ramos cells, CB-6644 (20 µM) interacts with the RUVBL1/2 complex[1]. With an EC50 range of 41 to 785 nM, CB-6644 (0.001-10 μM; 72 hours) potently kills 123 cell lines, including HCT116, NCI-1975, and HT29 cells[1].
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| ln Vivo |
CB-6644 (150 mg/kg, mouse model, SCID-beige mice adsorbed to Ramos xenograft model for 10 days, SCID-beige mice adsorbed to RPMI8226 xenograft model for 30 days) in individuals who have growing tumors In xenograft tumor models, it exhibits anti-tumor action; in the Ramos xenograft model and the RPMI8226 xenograft model, its tumor growth inhibition (TGI) is 68% and 81%, respectively [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: 123 cell lines such as HCT116, NCI-1975, and HT29 cells Tested Concentrations: 0.001, 0.01, 0.1, 1, and 10 μM Incubation Duration: 72 hrs (hours) Experimental Results: Potently killed cells with an EC50 range of 41 to 785 nM. |
| Animal Protocol |
Animal/Disease Models: SCID-beige mouse Burkitt lymphoma (Ramos) or multiple myeloma (RPMI8226) cell line with human tumor xenografts [1]
Doses: 150 mg/kg Route of Administration: One po (oral gavage) (one time/day) or twice (two times) daily (BID), Ramos treatment for 10 days, RPMI8226 treatment for 30 days. Experimental Results: There was no significant decrease in mouse body weight. The TGIs of Ramos and RPMI8226 are 68% and 81%, respectively. |
| References |
[1]. Assimon VA, et al. CB-6644 Is a Selective Inhibitor of the RUVBL1/2 Complex with Anticancer Activity. ACS Chem Biol. 2019 Feb 15;14(2):236-244.
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| Molecular Formula |
C₂₉H₃₄CLFN₄O₅
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| Molecular Weight |
573.06
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| CAS # |
2316817-88-4
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| SMILES |
COCC1=C(NC(CC(C)(C)CNC(C2=C(OCC)C=C(F)C(Cl)=C2)=O)=O)C(N(N1CCC3)C4=C3C=CC=C4)=O
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| Synonyms |
CB-6644CB 6644CB6644
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~174.50 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.63 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.63 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.63 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7450 mL | 8.7251 mL | 17.4502 mL | |
| 5 mM | 0.3490 mL | 1.7450 mL | 3.4900 mL | |
| 10 mM | 0.1745 mL | 0.8725 mL | 1.7450 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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