生物活性
DCC-2036 (Rebastinib)是一种Bcr-Abl抑制剂，作用于Abl1(WT)和Abl1(T315I)，IC50分别为0.8 nM和4 nM，也抑制SRC， LYN， FGR， HCK， KDR， FLT3，和Tie-2，对c-Kit具有低的抑制活性。
Targets
| Target | Value |
| u-Abl1(native) | IC50: 0.75nM |
| Abl1(H396P) | IC50: 1.4nM |
| p-Abl1(native) | IC50: 2nM |
| FLT3 | IC50: 2nM |
| p-Abl1(T315I) | IC50: 4nM |
| KDR | IC50: 4nM |
| u-Abl1(T315I) | IC50: 5nM |
| Tie-2 | IC50: 6nM |
| Lyn | IC50: 29nM |
| Src | IC50: 34nM |
| FGR | IC50: 38nM |
| Hck | IC50: 40nM |
| PDGFRα | IC50: 70nM |
| PDGFRβ | IC50: 113nM |
| c-Kit | IC50: 481nM |
| AuroraA | IC50: >5μM |
| CDK2/CyclinD | IC50: >5μM |
化学数据
| 目录号 | A11200 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 553.59 |
| Formula | C30H28FN7O3 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 1020172-07-9 |
| Synonyms | DCC2036 |
| SMILES | CC(C)(C)C1=NN(C(=C1)NC(=O)NC2=C(C=C(C=C2)OC3=CC(=NC=C3)C(=O)NC)F)C4=CC5=C(C=C4)N=CC=C5 |
溶解度
| In vitro (25°C) | DMSO | 103 mg/mL (186.05 mM) |
| Water | Insoluble |
| Ethanol | 15 mg/mL (27.09 mM) |
| In vivo | 0.5% CMC+0.25% Tween 80 | 15 mg/mL |
*<1 mg/ml means slightly soluble or insoluble.
*Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 18.06 mL | 90.32 mL | 180.64 mL |
| 0.5 mM | 3.61 mL | 18.06 mL | 36.13 mL |
| 1 mM | 1.81 mL | 9.03 mL | 18.06 mL |
| 5 mM | 0.36 mL | 1.81 mL | 3.61 mL |
*The above data is based on the productmolecular weight 553.59. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
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