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- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
Biological Activity
DCC-2036 is an orally bioavailable small-molecule inhibitor of multiple tyrosine kinases with potential antineoplastic activity.
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 |
| 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. |
|||
| 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.
| Catalog Num | A11200 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 1020172-07-9 |
| Formula | C30H28FN7O3 |
| M. Wt | 553.59 |
| Purity | >98% |
| 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 |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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