DCC-2036(Rebastinib)
Rebastinib(DCC-2036;DCC2036) is an inhibitor of tyrosine kinases TIE2 and ABL1.Rebastinib(DCC2036) can prevent primary tumor growth and lung metastasis in the PyMT breast cancer model. Rebastinib is approximately 50 times more potent as an inhibitor of TIE2 than BCR-ABL.
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Chemical Information
| Name | DCC-2036(Rebastinib) |
|---|---|
| Iupac Chemical Name | 1-(3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea |
| Synonyms | DCC-2036, Rebastinib, DCC2036, DCC 2036 |
| Molecular Formula | C30H28FN7O3 |
| Molecular Weight | 553.59 |
| Smile | C(C)(C)(C)C1=NN(C(=C1)NC(=O)NC1=C(C=C(C=C1)OC1=CC(=NC=C1)C(NC)=O)F)C=1C=C2C=CC=NC2=CC1 |
| InChiKey | WVXNSAVVKYZVOE-UHFFFAOYSA-N |
| InChi | InChI=1S/C30H28FN7O3/c1-30(2,3)26-17-27(38(37-26)19-7-9-23-18(14-19)6-5-12-33-23)36-29(40)35-24-10-8-20(15-22(24)31)41-21-11-13-34-25(16-21)28(39)32-4/h5-17H,1-4H3,(H,32,39)(H2,35,36,40) |
| CAS Number | 1020172-07-9 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | off-white solid |
|---|---|
| Purity | 98% |
| Storage | 3 years -20ºCpowder 6 months-80ºCin solvent |
| Solubility | 5mg/ml in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature |
| HS Code | 2933290090 |
| Targets | Rebastinib (DCC-2036) is a conformational control Bcr-Abl inhibitor for Abl1WT and Abl1T315I with IC50 of 0.8 nM and 4 nM, also inhibits SRC, KDR, FLT3, and Tie-2, and low activity to seen towards c-Kit. |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1. Anthony W. Tolcher, Pamela N. Munster, Lee S. Rosen, Curran Murphy, Christian Argueta, Keisuke Kuida, Rodrigo Ruiz-Soto, Filip Janku, An open label, multicenter, phase 1b/2 study of rebastinib (DCC-2036) in combination with carboplatin to assess safety, tolerability, and pharmacokinetics in patients with advanced or metastatic solid tumors. DOI:10.1200/JCO.2019.37.15_suppl.TPS2666 Journal of Clinical Oncology 37, no. 15_suppl Published online May 26, 2019.
Chemical Structure
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