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My CartCAS：649735-46-6
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 649735-46-6 |
| Name | Brivanib |
| Molecular Formula | C19H19FN4O3 |
| Molecular Weight | 370.39 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD13194684 |
| SMILES | FC1=C(OC2=NC=NN3C2=C(C(OC[C@H](O)C)=C3)C)C=CC4=C1C=C(C)N4 |
| Target Point | VEGFR2/KDR/Flk-1;FGFR2 |
| Passage | Angiogenesis; Protein Tyrosine Kinase/RTK |
| Background | Brivanib is an ATP-competitive VEGFR2 inhibitor. |
| Biological Activity | Brivanib 是一种ATP竞争性的 VEGFR2 抑制剂，IC50 值为 25 nM；可以适度抑制 VEGFR-1 和 FGFR-1，对 VEGFR2 的选择性是对 PDGFR-β 的 240 倍[1-3]。 |
| IC50 | VEGFR2:25nM [1-3] |
| In Vitro | Brivanib抑制VEGFR1和FGFR-1，IC50为0.38μM和0.148μM。 Brivanib对PDGFRβ，EGFR，LCK，PKCα或JAK-3不敏感，IC50均高于1900 nM。 Brivanib可以抑制VEGF刺激的HUVEC的增殖，IC50为40 nM，而FGF刺激的HUVEC中为276 nM。另一方面，brivanib对肿瘤细胞系表现出低活性[1]。 Brivanib剂量≤20μM反常增强FGF诱导的LX-2细胞增殖，而较高的brivanib剂量(≥30μM)抑制LX-2细胞增殖。 brivanib对肝纤维化的抑制作用不是通过抑制TGF-β1诱导的星状细胞活化，而是可能通过抑制PDGF-BB诱导的星状细胞活化[3]。 |
| In Vivo | Brivanib在无胸腺小鼠的H3396异种移植物中显示出抗肿瘤活性。在剂量为60和90 mg/kg(po)时，brivanib完全抑制肿瘤生长，TGI分别为85％和97％[1]。此外，brivanib显著抑制肝细胞癌(HCC)异种移植物中的肿瘤生长，这是由于VEGFR2的磷酸化降低。结果显示06-0606异种移植小鼠的肿瘤重量分别为55％和13％，与对照组相比，剂量为50mg/kg和100mg/kg。建议Brivanib有效治疗HCC [2]。 Brivanib(50mg/kg，po)减弱小鼠中由BDL诱导的肝纤维化和星状细胞活化。 Brivanib抑制假对照动物的生长因子和生长因子受体mRNA表达，但在胆管结扎动物中表现出不同的作用[3]。 |
| Cell Experiment | 使用细胞计数试剂盒-8(CCK-8)在LX-2细胞中测量活力。使用每孔2，000个细胞的96孔板，将HSC在10％FBS补充的DMEM中孵育24小时，然后在无血清培养基中饥饿。饥饿24小时后，以不同剂量加入brivanib。两小时后，加入5ng/mL PDGF-BB。将细胞再孵育72小时并测量细胞活力。每个实验重复进行三次，至少四次。 |
| Animal Experiment | 4-6周龄的雄性小鼠每周处理3次，总共12次腹膜内(ip)注射150mL/kg TAA。在TAA治疗开始时，安慰剂或brivanib(25或50mg/kg)连续5天口服给药，周末休息。在注射开始后4周处死动物。 |
| Data Literature Source | [1]. Bhide RS，et al. Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2，1-f][1，2，4]triazin-6-yloxy)propan- 2-ol (BMS-540215)，an in vivo active potent VEGFR-2 inhibitor. J Med Chem，2006，49 (7)，2143-2146. [2]. Huynh H，et al. Brivanib alaninate，a dual inhibitor of vascular endothelial growth factor receptor and fibroblast growth factor receptor tyrosine kinases，induces growth inhibition in mouse models of human hepatocellular carcinoma. Clin Cancer Res，2008， [3]. Nakamura I，et al. Correction: Brivanib Attenuates Hepatic Fibrosis In Vivo and Stellate Cell Activation In Vitro by Inhibition of FGF，VEGF and PDGF Signaling. PLoS One. 2015 Nov 3;10(11):e0142355 |
| Unit | Bottle |
| Specification | 2mg 5mg 10mg |
是一种ATP竞争性的 VEGFR2 抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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