Home > Axl & c-Met & FLT3 & VEGFR & VEGFR & > Cabozantinib

Cabozantinib

卡博替尼,卡赞替尼,博卡替尼,XL184,BMS-907351,XL 184,BMS 907351,XL-184,BMS907351

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。

目录号
EY1204
EY1204
EY1204
纯度
99.17%
99.17%
99.17%
规格
5 mg
10 mg
50 mg
原价
750
1000
2600
售价
750
1000
2600
库存
现货
现货
现货
订购
订购
订购
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  • 生物活性

    Cabozantinib (XL184, BMS-907351) is an orally active, potent inhibitor of VEGFR2 with IC50 of 0.035 nM. Cabozantinib also inhibits c-Met, Kit, VEGFR3, Axl, FlT3, VEGFR1 and Tie-2 with IC50 of 1.3 nM, 4.6 nM, 6.0 nM, 7.0 nM, 11.3 nM, 12 nM and 14.3 nM, respectively.

  • 体外研究

  • 体内研究

    30% propylene glycol, 5% Tween 80, 65% D5W(5%葡萄糖水溶液)

  • 激酶实验

  • 细胞实验

    ~10 μM

  • 动物实验

    ~60 mg/kg 口服饲喂

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] You WK, et al. Cancer Res, 2011, 71(14), 4758-4768.
    [2] Yakes et al (2011) Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol.Cancer Ther. 10 2298.

    分子式
    C28H24FN3O5    		 分子量
    501.51    		 CAS号
    849217-68-1    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    100 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02101736 NF1|Neurofibromatosis|Plexiform Neurofibromas Drug: Cabozantinib University of Alabama at Birmingham Phase 2 2014-06-01 2016-09-26
    NCT01834651 Prostate Cancer Drug: Cabozantinib Edwin Posadas, MD|Cedars-Sinai Medical Center Phase 2 2013-04-01 2016-12-29
    NCT01954745 Bile Duct Cancer|Intrahepatic Cholangiocarcinoma|Cholangiocarcinoma of the Extrahepatic Bile Duct Drug: Cabozantinib Massachusetts General Hospital|Exelixis Phase 2 2013-09-01 2016-12-12
    NCT02008383 Colorectal Cancer Biological: Panitumumab|Drug: Cabozantinib John Strickler, M.D.|Exelixis|Duke University Phase 1 2014-01-01 2016-09-17
    NCT02302833 Neuroendocrine Tumors Drug: Cabozantinib|Behavioral: Questionnaire M.D. Anderson Cancer Center|Exelixis Phase 2 2015-02-01 2017-03-07
    NCT02036476 Merkel Cell Carcinoma|Skin Cancer Drug: Cabozantinib Dana-Farber Cancer Institute|Exelixis Phase 2 2014-01-01 2016-09-09
    NCT01553656 Solid Tumors|Cancer|NSCLC Drug: cabozantinib capsules|Drug: cabozantinib tablets Exelixis Phase 1 2011-02-01 2015-08-19
    NCT01428219 Prostate Cancer Metastatic Drug: Cabozantinib University of Michigan Cancer Center|Exelixis Phase 2 2012-02-01 2016-03-29
    NCT01588821 Lung Cancer|Solid Tumor (Not Breast or Prostate Cancers) Drug: Cabozantinib Massachusetts General Hospital Phase 2 2012-06-01 2016-09-12
    NCT01738438 Breast Cancer Drug: Cabozantinib Dana-Farber Cancer Institute Phase 2 2013-02-01 2016-10-24
    NCT01582295 Multiple Myeloma Drug: Cabozantinib Massachusetts General Hospital Phase 1 2012-06-01 2017-02-25
    NCT01908426 Hepatocellular Carcinoma Drug: Cabozantinib tablets|Drug: Placebo tablets Exelixis Phase 3 2013-08-01 2016-08-04
    NCT01709435 Childhood Solid Neoplasm|Childhood Thyroid Gland Medullary Carcinoma|Recurrent Childhood Central Nervous System Neoplasm|Recurrent Malignant Solid Neoplasm|Recurrent Melanoma|Recurrent Thyroid Gland Carcinoma Drug: Cabozantinib S-malate|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study National Cancer Institute (NCI) Phase 1 2012-11-01 2017-03-20
    NCT01961765 Relapsed Acute Myeloid Leukemia|Refractory Acute Myeloid Leukemia Drug: cabozantinib Massachusetts General Hospital|Exelixis Phase 1 2013-11-01 2017-02-15
    NCT01493869 Healthy|Hepatic Impairment Drug: cabozantinib Exelixis Phase 1 2011-09-01 2014-09-19
    NCT01663272 Pancreatic Cancer Drug: CABOZANTINIB|Drug: gemcitabine University of Michigan Cancer Center Phase 1 2012-07-01 2016-03-18
    NCT01639508 Non-Small Cell Lung Cancer Drug: Cabozantinib Memorial Sloan Kettering Cancer Center|Exelixis Phase 2 2012-07-01 2017-02-13
    NCT01605227 Prostate Cancer|Castration Resistant Prostate Cancer|Pain|Prostatic Neoplasms Drug: cabozantinib|Drug: prednisone Exelixis Phase 3 2012-06-01 2015-04-13
    NCT01630590 Prostate Cancer Drug: Cabozantinib|Drug: Androgen Ablation Therapy M.D. Anderson Cancer Center|Exelixis|High Impact Clinical Research Support Program Phase 2 2014-01-08 2017-03-23
    NCT01865747 Renal Cell Carcinoma Drug: Cabozantinib tablets|Drug: Everolimus (Afinitor) tablets Exelixis Phase 3 2013-06-01 2016-07-14
    NCT01866293 Relapsed or Refractory Multiple Myeloma Drug: Cabozantinib (XL184) Memorial Sloan Kettering Cancer Center|Exelixis Phase 1|Phase 2 2013-05-28 2017-02-08
    NCT01822522 Advanced Malignant Solid Neoplasm|HIV Infection|Metastatic Malignant Solid Neoplasm|Recurrent Malignant Solid Neoplasm|Unresectable Solid Neoplasm Drug: Cabozantinib S-malate|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study National Cancer Institute (NCI) Phase 1 2013-06-01 2017-03-20
    NCT01441947 Breast Cancer Drug: Cabozantinib|Drug: Fulvestrant Massachusetts General Hospital|Exelixis Phase 2 2011-10-01 2016-10-23
    NCT01703065 Adenocarcinoma of the Prostate|Castration-resistant Prostate Cancer|Recurrent Prostate Cancer|Stage III Prostate Cancer|Stage IV Prostate Cancer Drug: cabozantinib-s-malate|Other: laboratory biomarker analysis University of Washington|Prostate Cancer Foundation|National Cancer Institute (NCI) 2013-06-18 2017-02-21
    NCT01466036 Carcinoid Tumor|Pancreatic Neuroendocrine Tumor Drug: Cabozantinib Massachusetts General Hospital Phase 2 2012-07-01 2016-09-14

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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