1020172-07-9
DCC-2036 (Rebastinib)
CAS: 1020172-07-9
Molecular Formula: C30H28FN7O3
1020172-07-9 - Names and Identifiers
| Name | DCC-2036 (Rebastinib) |
| Synonyms | DCC2036 CS-1867 DCC 2036 Rebastinib Rebastinib(DCC-2036) DCC-2036 (Rebastinib) N-[3-tert-Butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]-N'-[2-fluoro-4-[(2-(MethylcarbaMoyl)pyridin-4-yl) 1-(3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea N-[3-tert-Butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]-N'-[2-fluoro-4-[(2-(methylcarbamoyl)pyridin-4-yl)oxy]phenyl]urea N-[3-tert-Butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]-N'-[2-fluoro-4-[(2-(methylcarbamoyl)pyridin-4-yl)oxy]phenyl]urea DCC-2036 (Rebastinib) |
| CAS | 1020172-07-9 |
1020172-07-9 - Physico-chemical Properties
| Molecular Formula | C30H28FN7O3 |
| Molar Mass | 553.59 |
| Density | 1.32 |
| Melting Point | >181°C (dec.) |
| Boling Point | 666.8±55.0 °C(Predicted) |
| Solubility | Methanol (Slightly) |
| Appearance | Solid |
| Color | Off-White |
| pKa | 12.25±0.70(Predicted) |
| Storage Condition | -20°C Freezer |
| In vitro study | DCC-2036 effective inhibition of purified unphosphorylated (u-ABL1native) and phosphorylated (p-ABL1native) ABL1, unphosphorylated and phosphorylated mutant ABL1T315I, and activating loop mutation ABL1H396P, which is non-ATP competitive, the IC50 values were 0.8 nM, 2 nM, 1.4 nM, 5 nM, and 4 nM, respectively. Moreover, DCC-2036 also inhibited the SRC family kinases SRC, LYN, FGR, and HCK, and the receptors TKs KDR, FLT3, and TIE2, with IC50 of 34 nM, 29 nM, 38 nM, 40 nM, 4 nM, 2 nM and 6 nM. DCC-2036 acts on Ba/F3 cells expressing either wild-type or mutant BCR-ABL1 with Antiproliferative activity with an IC50 of 2 nM to 150 nM. In addition, DCC-2036 also inhibited proliferation of Ph cell line K562(IC50 5.5 nM) and effectively induced apoptosis of Ba/F3 and K562 cells expressing BCR-ABL1. Recent studies have shown that DCC-2036 selectively inhibits BCR-ABL positive cells by significantly inhibiting CML cell lines compared to non-CML leukemia cell lines. DCC-2036 potent inhibition of purified unphosphorylated (u-ABL1 recent studies show DCC-2036 selective inhibition of BCR-ABL positive cells by significant inhibition of CML cell lines compared to non-CML leukemia cell lines). |
| In vivo study | DCC-2036, the mice with Ba/F3-BCR-ABL1T315I leukemia cells were orally fed with a dose of 100 mg/kg per day, and the transplanted tumor model was effectively inhibited by BCR-ABL1 signal once a day, and the life of the mice was significantly prolonged. In DCC-2036, the mice with Ba/F3-BCR-ABL1T315I leukemia cells were orally fed with 100 mg/kg dose once a day to effectively inhibit the BCR-ABL1 signal, and significantly prolong the life of mice. |
1020172-07-9 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.806 ml | 9.032 ml | 18.064 ml |
| 5 mM | 0.361 ml | 1.806 ml | 3.613 ml |
| 10 mM | 0.181 ml | 0.903 ml | 1.806 ml |
| 5 mM | 0.036 ml | 0.181 ml | 0.361 ml |
Last Update：2024-01-02 23:10:35
Supplier List
Product Name: DCC-2036 (Rebastinib) Visit Supplier Webpage Request for quotation
CAS: 1020172-07-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1020172-07-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Product Name: DCC-2036 (Rebastinib) Visit Supplier Webpage Request for quotation
CAS: 1020172-07-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1020172-07-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History