酪氨酸激酶抑制剂(TYROSINE KINASE INHIBITOR)
Brivanib (BMS-540215)
CAS: 649735-46-6
Molecular Formula: C19 H19 F N4 O3
酪氨酸激酶抑制剂(TYROSINE KINASE INHIBITOR) - Names and Identifiers
酪氨酸激酶抑制剂(TYROSINE KINASE INHIBITOR) - Physico-chemical Properties
| Molecular Formula | C19 H19 F N4 O3 |
| Molar Mass | 370.38 |
| Density | 1.42 |
| Solubility | Soluble in DMSO (74 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (3 mg/m |
| Appearance | Yellow powder. |
| pKa | 14.18±0.20(Predicted) |
| Storage Condition | -20℃ |
| Use | An ATP-competitive inhibitor against VEGFR-2, Flk-1, VEGFR-1 and FGFR-1 |
| In vitro study | Brivanib also inhibited VEGFR-1 and FGFR-1 with IC50 of 0.38 and 0.148 μm, respectively. Brivanib has little effect on PDGFR-β, EGFR, LCK, pkcα or JAK-3, and IC50 is greater than 1900 nM. Brivanib inhibited the proliferation of VEGF-stimulated HUVECs cells with an IC50 of 40 nM and acted on the proliferation of FGF-stimulated HUVECs cells with an IC50 of 276 nM. On the other hand, Brivanib has low cytotoxicity on tumor cell lines. |
| In vivo study | Brivanib has anti-cancer activity against athymic mice bearing H3396 xenografts. Oral treatment with Brivanib at doses of 60 and 90 mg/kg resulted in completely consistent tumor growth with TGI of 85% and 97%, respectively. Furthermore, Brivanib significantly inhibited the growth of hepatocellular xenograft tumors by reducing phosphorylation by VEGFR-2. The results showed that the body weights of the mice bearing the 06-0606 xenografts were 100 and 55%, respectively, compared to the control histamine 50 mg/kg and 13% mg/kg dose treatments. Brivanib is very effective in the treatment of HCC. |
酪氨酸激酶抑制剂(TYROSINE KINASE INHIBITOR) - Introduction
Brivanib (BMS-540215) is an ATP competitive VEGFR2 inhibitor with IC50 of 25 nM. It has moderate inhibitory effect on VEGFR-1 and FGFR-1, but it is more than 240 times stronger than PDGFR-β.
Last Update：2022-10-16 17:41:45
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View History
酪氨酸激酶抑制剂(TYROSINE KINASE INHIBITOR)
2-Iodobenzoic acid chloride
Selenium(IV) dioxide
(1-甲基-3-三氟甲基-1H-吡唑-4-基)甲胺
2-PHENYLETHYL SS-D-THIOGALACTOSIDE
2-Iodobenzoic acid chloride
Selenium(IV) dioxide
(1-甲基-3-三氟甲基-1H-吡唑-4-基)甲胺
2-PHENYLETHYL SS-D-THIOGALACTOSIDE