| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| C408163-1ml |
1ml |
现货  |
|
| 别名 | 苹果酸卡博替尼（XL184） |
|---|---|
| 英文别名 | Butanedioic acid, 2-hydroxy-, (2S)-, compd. with N-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide (1:1) |
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | Cabozantinib malate (XL184) |
| 生化机理 | Cabozantinib苹果酸盐（XL184）是Cabozantinib的苹果酸盐，Cabozantinib是一种强效VEGFR2抑制剂，IC50为0.035 nM，还能抑制c-Met、Ret（c-Ret）、Kit（c-Kit）、Flt-1/3/4、Tie2和AXL，在无细胞实验中的IC50分别为1.3 nM、4 nM、4.6 nM、12 nM/11.3 nM/6 nM、14.3 nM和7 nM。苹果酸卡博替尼（XL184）可诱导细胞凋亡。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 肝细胞生长因子受体抑制剂 |
| 产品介绍 |
Cabozantinib malate (XL184)是Cabozantinib的苹果酸盐，是有效的VEGFR2抑制剂，IC50为0.035 nM，也抑制c-Met， Ret， Kit， Flt-1/3/4， Tie2和AXL，IC50分别为1.3 nM， 4 nM， 4.6 nM， 12 nM/11.3 nM/6 nM， 14.3 nM和7 nM。 Information Cabozantinib malate (XL184) is the malate of Cabozantinib, a potentVEGFR2inhibitor withIC50of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-Kit), Flt-1/3/4, Tie2, and AXL withIC50of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cel Cabozantinib has weak inhibitory activity against RON and PDGFRβ with IC50 of 124 nM and 234 nM, respectivey, and has low activity against FGFR1 with IC50 of 5.294 μM. Cabozantinib at low concentration (0.1-0.5 μM) is sufficient to induce marked inhibition of constitutive and inducible Met phosphorylation and its resultant downstream signaling in MPNST cells, and inhibit HGF-induced MPNST cell migration and invasion. Cabozantinib also induces marked inhibition of Met and VEGFR2 phosphorylation in cytokine-stimulated human umbilical vein endothelial cells (HUVECs). Although Cabozantinib has no significant effect on MPNST cell growth at 0.1 μM, Cabozantinib at 5-10 μM significantly inhibits the MPNST cell growth. In vivo Cabozantinib treatment at 30 mg/kg in RIP-Tag2 mice with spontaneous pancreatic islet tumors disrupts 83% of the tumor vasculature, reduces pericytes and empty basement membrane sleeves, causes widespread intratumoral hypoxia and extensive tumor cell apoptosis, and slows regrowth of the tumor vasculature after drug withdrawal, more significantly compared with XL999 that blocks VEGFR but not c-Met, leading to only 43% reduction in vascularity, suggesting that concurrent inhibition of VEGFR and other functionally relevant receptor tyrosine kinases (RTK) amplifies angiogenesis inhibition. Cabozantinib also decreases invasiveness of primary tumors and reduces metastasis. Cabozantinib at 30 mg/kg/day significantly abrogates human MPNST xenografts growth and metastasis in SCID mice. Administration of Cabozantinib induces dose-dependent inhibition of tumor growth in breast, lung, and glioma tumor models, in association with decreased tumor and endothelial cell proliferation as well as increased apoptosis. A single oral dose of Cabozantinib is sufficient to induce sustained tumor growth inhibition in MDA-MB-231 tumor-bearing mice and C6 tumor-bearing rats at 100 mg/kg and 10 mg/kg, respectively. cell lines： Concentrations：Dissolved in DMSO, final concentrations ~10 μM Incubation Time：48 hours Powder Purity:≥99% |
| IC50 | VEGFR2/KDR, IC50: 0.035 nM |
|---|---|
| ALogP | 3.331 |
| hba_count | 8 |
| HBD Count | 3 |
| Rotatable Bond | 11 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | COC1=CC2=C(C=C1OC)C(=CC=N2)OC3=CC=C(NC(=O)C4(CC4)C(=O)NC5=CC=C(F)C=C5)C=C3.OC(CC(O)=O)C(O)=O |
| 分子量 | 635.59 |
| Reaxy-Rn | 20538690 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=20538690&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 30 mg/mL (92.09 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|---|
| DMSO(mg / mL) Max Solubility | 100 |
| DMSO(mM) Max Solubility | 157.33 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 20538690 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=20538690&ln= |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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