Cabozantinib (XL184, BMS-907351)
目录号：S1119
Molecular Weight(MW): 501.51
Cabozantinib (XL184, BMS-907351)是一种有效的VEGFR2抑制剂，在无细胞试验中IC50为0.035 nM，也能有效抑制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。
客户使用该产品的6个实验数据：
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Effects of AXL inhibitors on induction of pAKT and rescue of pERK following AXL overexpression. R428, 500 nmol/L; XL184, 3 umol/L; XL880, 100 nmol/L; in the presence or absence of 2 umol/L PLX4720. shAXL is a positive control.
Cancer Discov 2014 4(7), 816-27. Cabozantinib (XL184, BMS-907351) purchased from Selleck.
Imaging and quantification of cabozantinib (XL-184) effects on EMT in vitro. A-C, Western blot analysis of E-cadherin and c-Met expression in the XL-184-treated RFPþ tumor cells. D-F, GFP imaging merged with bright field view of the XL-184–treated RFPþ tumor cells.
Cancer Res, 2016, 76(8):2094-104. Cabozantinib (XL184, BMS-907351) purchased from Selleck.
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Cabozantinib specifically inhibited the phosphorylation of FLT3 (A) and downstream signaling molecules such as STAT5, Akt and ERK1/2 in FLT3-ITD MV4-11 cells (B). By contrast, the phosphorylation of downstream FLT3 signaling molecules was unaffected by cabozantinib in FLT3 wild-type OCI-AML3 cells (C). Cells were treated with cabozantinib for 2 h, and the expression of pFLT3, FLT3, pSTAT5, STAT5, pAkt, Akt, pErk1/2, and Erk1/2 was measured by Western blotting.
Cancer Lett, 2016, 376(2):218-25. Cabozantinib (XL184, BMS-907351) purchased from Selleck.
Cabozantinib reduces viability and spheroid and colony formation of GCTB stromal cells. (a) Adherent-growing GCTB stromal cells derived from three different patients were left untreated (CO) or were treated with cabozantinib (10 uM, XL184) or methotrexate (100 uM, MTX). Seventy-two hours later, the viability was measured by the MTT assay, and the control was set to 100%. (b) Spheroidal cultures were established as described in b. After spheroid formation, the cells were left untreated or were treated as described above. Seven days later, spheroids were photographed, and the number and volume of spheroids (spheroid surface) were determined. The data shown are the MD. (*P<0.05; **P<0.01).
Cell Death Dis 2014 5, e1471. Cabozantinib (XL184, BMS-907351) purchased from Selleck.
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The effect of cabozantinib on the accumulation of Dox and Rho123. (A) Fluorescence microscopy observation of the accumulation of Dox and Rho123. The scale bars represent 100 uM. (B) The accumulation of Dox and Rho123 was measured by flow cytometric analysis. The data were analysed using Kaluza software and are presented as fold-change in fluorescence intensity relative to the control HepG2/adr cells. The results are shown as the mean ± SD of three independent trials. *P < 0.05 vs. the control group.
Liver Int 2014 10.1111/liv.12524. Cabozantinib (XL184, BMS-907351) purchased from Selleck.
Inhibition of breast cancer cell growth using XL184. MCF-7 breast cancer cells were treated with increasing concentrations of XL-184 for 5 days. Cell number was measured using a colorimetric growth assay (crystal violet stain) and expressed relative to DMSO treated control cells.
Christina W Yde/CDM Danish Cancer Society Research Center Denmark. Cabozantinib (XL184, BMS-907351) purchased from Selleck.
产品安全说明书
VEGFR抑制剂选择性比较
生物活性
| 产品描述 | Cabozantinib (XL184, BMS-907351)是一种有效的VEGFR2抑制剂，在无细胞试验中IC50为0.035 nM，也能有效抑制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。 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 体外研究 |
XL184是多种受体酪氨酸激酶小分子抑制剂，尤其抑制c-Met 和VEGFR2。XL-184也有效作用于Ret, Kit, FLT1, FLT3, FLT4, Tie2, 和 AXL ， IC50分别为 4 nM, 4.6 nM, 12 nM, 11.3 nM, 6 nM, 14.3 nM, 和7 nM。XL184微弱抑制 RON 和PDGFR-β，IC50分别为 124 nM和 234 nM,而对FGFR1则几乎没有抑制活性，IC50 为5.294 μM。[1] XL184低浓度(0.1-0.5 μM) 时处理MPNST细胞，也显著抑制组成型和诱导型Met磷酸化及其下游信号，且抑制 HGF诱导的MPNST细胞迁移和侵袭。XL184作用于细胞因子刺激的人脐静脉内皮细胞（HUVECs），也显著抑制Met和VEGFR2磷酸化。虽然XL184浓度为0.1 μM时不能抑制MPNST细胞生长，但是浓度为5-10 μM 时则能显著抑制MPNST细胞生长。[2] |
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| Cell Data |
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| 体内研究 | XL184按 30 mg/kg 剂量处理携带自发胰岛细胞瘤的RIP-Tag2 小鼠，扰乱 83%肿瘤血管, 降低周细胞和空基底膜袖，引起广泛瘤内缺氧和广泛的肿瘤细胞凋亡，且停药后延缓肿瘤血管再生长，与XL999相比更显著抑制VEGFR而不是c-Met，导致血管降低43％，说明抑制VEGFR，也抑制放大抑制血管新生的其他功能相关的受体酪氨酸激酶（RTK）。XL184也降低原发肿瘤的侵袭和减少转移。[1] XL184 每天按30 mg/kg剂量处理SCID小鼠，显著废除人 MPNST移植瘤生长和转移。[2] XL184 处理乳腺癌，肺癌胶质瘤模型，抑制肿瘤生长，这种作用存在剂量依赖性，降低肿瘤和内皮细胞增殖，促进凋亡。XL184按100 mg/kg 和 10 mg/kg剂量分别单独处理携带MDA-MB-231肿瘤的小鼠和携带C6肿瘤的大鼠，持续抑制肿瘤生长。[3] |
推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)
| 细胞实验： [2] |
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| 动物实验：[1] |
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溶解度 (25°C)
| 体外 | DMSO | 100 mg/mL (199.39 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble | |
| 体内 |
从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 2% DMSO+30% PEG 300+5% Tween 80+ddH2O |
5mg/mL |
* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。
化学数据
| 分子量 | 501.51 |
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| 化学式 | C28H24FN3O5 |
| CAS号 | 849217-68-1 |
| 稳定性 | powder |
| in solvent | |
| 别名 | N/A |
计算器
摩尔浓度计算器
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。
稀释计算器
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )
在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.
分子量计算器
通过输入化合物的化学式来计算其分子量：
注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2
摩尔浓度计算器
临床试验信息
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03586973 | Recruiting | Advanced Hepatocellular Carcinoma | Takeda | July 9 2018 | Phase 2 |
| NCT02496208 | Recruiting | Bladder Small Cell Neuroendocrine Carcinoma|Clear Cell Renal Cell Carcinoma|Infiltrating Bladder Urothelial Carcinoma Sarcomatoid Variant|Infiltrating Bladder Urothelial Carcinoma Plasmacytoid Variant|Kidney Medullary Carcinoma|Metastatic Malignant Neoplasm in the Bone|Metastatic Penile Carcinoma|Metastatic Renal Cell Carcinoma|Renal Pelvis Urothelial Carcinoma|Sarcomatoid Renal Cell Carcinoma|Squamous Cell Carcinoma of the Penis|Stage III Bladder Adenocarcinoma AJCC v6 and v7|Stage III Bladder Squamous Cell Carcinoma AJCC v6 and v7|Stage III Bladder Urothelial Carcinoma AJCC v6 and v7|Stage III Penile Cancer AJCC v7|Stage III Renal Cell Cancer AJCC v7|Stage III Renal Pelvis Cancer AJCC v7|Stage III Ureter Cancer AJCC v7|Stage III Urethral Cancer AJCC v7|Stage IIIa Penile Cancer AJCC v7|Stage IIIb Penile Cancer AJCC v7|Stage IV Bladder Adenocarcinoma AJCC v7|Stage IV Bladder Squamous Cell Carcinoma AJCC v7|Stage IV Bladder Urothelial Carcinoma AJCC v7|Stage IV Penile Cancer AJCC v7|Stage IV Renal Cell Cancer AJCC v7|Stage IV Renal Pelvis Cancer AJCC v7|Stage IV Ureter Cancer AJCC v7|Stage IV Urethral Cancer AJCC v7|Ureter Urothelial Carcinoma|Urethral Urothelial Carcinoma | National Cancer Institute (NCI) | July 9 2015 | Phase 1 |
| NCT02867592 | Recruiting | Adrenal Cortex Carcinoma|Alveolar Soft Part Sarcoma|Central Nervous System Neoplasm|Childhood Clear Cell Sarcoma of Soft Parts|Clear Cell Sarcoma of Soft Tissue|Ewing Sarcoma|Hepatoblastoma|Hepatocellular Carcinoma|MITF Positive|Osteosarcoma|Recurrent Adrenal Cortex Carcinoma|Recurrent Alveolar Soft Part Sarcoma|Recurrent Ewing Sarcoma|Recurrent Hepatoblastoma|Recurrent Hepatocellular Carcinoma|Recurrent Malignant Central Nervous System Neoplasm|Recurrent Malignant Solid Neoplasm|Recurrent Osteosarcoma|Recurrent Renal Cell Carcinoma|Recurrent Rhabdomyosarcoma|Recurrent Soft Tissue Sarcoma|Recurrent Soft Tissue Sarcoma Excluding Rhabdomyosarcoma|Recurrent Thyroid Gland Medullary Carcinoma|Refractory Ewing Sarcoma|Refractory Malignant Central Nervous System Neoplasm|Refractory Malignant Solid Neoplasm|Refractory Osteosarcoma|Refractory Rhabdomyosarcoma|Refractory Soft Tissue Sarcoma|Refractory Soft Tissue Sarcoma Excluding Rhabdomyosarcoma|Renal Cell Carcinoma|Rhabdomyosarcoma|Soft Tissue Sarcoma Excluding Rhabdomyosarcoma|Solid Neoplasm|Thyroid Gland Medullary Carcinoma|Wilms Tumor | National Cancer Institute (NCI) | May 8 2017 | Phase 2 |
| NCT01630590 | Active not recruiting | Prostate Cancer | M.D. Anderson Cancer Center|Exelixis|High Impact Clinical Research Support Program | January 8 2014 | Phase 2 |
| NCT01835158 | Active not recruiting | Clear Cell Renal Cell Carcinoma|Metastatic Renal Cell Cancer|Stage III Renal Cell Cancer AJCC v7|Stage IV Renal Cell Cancer AJCC v7 | National Cancer Institute (NCI) | July 8 2013 | Phase 2 |
| NCT01811212 | Completed | Poorly Differentiated Thyroid Gland Carcinoma|Recurrent Thyroid Gland Carcinoma|Stage I Thyroid Gland Follicular Carcinoma|Stage I Thyroid Gland Papillary Carcinoma|Stage II Thyroid Gland Follicular Carcinoma|Stage II Thyroid Gland Papillary Carcinoma|Stage III Thyroid Gland Follicular Carcinoma|Stage III Thyroid Gland Papillary Carcinoma|Stage IVA Thyroid Gland Follicular Carcinoma|Stage IVA Thyroid Gland Papillary Carcinoma|Stage IVB Thyroid Gland Follicular Carcinoma|Stage IVB Thyroid Gland Papillary Carcinoma|Stage IVC Thyroid Gland Follicular Carcinoma|Stage IVC Thyroid Gland Papillary Carcinoma|Tall Cell Variant Thyroid Gland Papillary Carcinoma|Thyroid Gland Oncocytic Follicular Carcinoma | National Cancer Institute (NCI)|Exelixis | May 8 2013 | Phase 2 |
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