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CCT251236 is a cell-based phenotypic high-throughput screening (HTS) chemical probe developed to screen for inhibitors of the HSF1 stress pathway.CCT251236 exhibits antimyeloma activity and inhibits HSF1.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $31 | - | In Stock | |
| 5 mg | $113 | - | In Stock | |
| 10 mg | $222 | - | In Stock | |
| 25 mg | $459 | - | In Stock | |
| 50 mg | $735 | - | In Stock | |
| 100 mg | $1,170 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $139 | - | In Stock |
| Description | CCT251236 is a cell-based phenotypic high-throughput screening (HTS) chemical probe developed to screen for inhibitors of the HSF1 stress pathway.CCT251236 exhibits antimyeloma activity and inhibits HSF1. |
| Targets&IC50 | HSP72:19 nM |
| In vitro | CCT367766 (0-100 nM; 24 hours) inhibited 17-AAG-induced HSF1-mediated expression of heat shock proteins HSP72 and HSP27 in SK-OV-3 cells in a concentration-dependent manner; CCT367766 also blocked 17-AAG-induced HSPA1A mRNA in a dose-dependent manner; in addition, CCT367766 (0-100 nM; 24 hours) exhibited an ideal balance of in vitro properties while maintaining good cell viability, with pIC50=7.73±0.07 (IC50=19 nM) for inhibiting HSF1-mediated HSP72 induction; in SK-OV-3 cells, the free GI50 was 1.1 nM[1]. |
| In vivo | CCT367766 (oral; 20 mg/kg; 33 days) showed significant efficacy in mice, with a tumor growth inhibition (%TGI) of 70% based on final tumor volume.After 33 days, there was a 64% reduction in mean tumor weight compared to controls. In addition, the basicity and high volume of distribution of the compound was observed in tumors up to a concentration of 940 nM [1].CCT367766 (oral, 5 or 20 mg/kg) showed free Cav0-24h values of 2.0 nM and 1.2 nM, respectively, in tumor-free immune-competent BALB/c mice [1]; and, in a mouse model of human myeloma xenografts, the CCT251236 (20 mg/kg, po) inhibited the HSF1 pathway and exhibited antimyeloma efficacy in a human myeloma xenograft mouse model [2]. |
| Molecular Weight | 552.62 |
| Formula | C32H32N4O5 |
| Cas No. | 1693731-40-6 |
| Smiles | Cc1ccc(NC(=O)c2ccc3OCCOc3c2)cc1NC(=O)c1ccc2nc(OCCN3CCCC3)ccc2c1 |
| Relative Density. | 1.328 g/cm3 (Predicted) |
| Color | White |
| Appearance | Solid |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (144.76 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (5.97 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
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DMSO
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