Home > VEGFR & VEGFR & > Cabozantinib malate

Cabozantinib malate

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

Cabozantinib S-malate (XL184, BMS-907351)是高活性VEGFR2抑制剂，IC50为 0.035 nM，同时对c-Met，Ret，Kit，Flt-1/3/4，Tie2和AXL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。

目录号
EY1026
EY1026
EY1026
EY1026
纯度
99.56%
99.56%
99.56%
99.56%
规格
5 mg
10 mg
50 mg
100 mg
原价
500
770
980
1520
售价
500
770
980
1520
库存
现货
现货
现货
现货
订购
订购
订购
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  • 生物活性

    Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    溶解于DMSO，~10 μM

  • 动物实验

    ~60 mg/kg 口服强饲

  • 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.

    分子式
    C32H30FN3O10    		 分子量
    635.59    		 CAS号
    1140909-48-3    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    98 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
    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
    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
    NCT02867592 Adrenal Cortex Carcinoma|Adult Alveolar Soft Part Sarcoma|Adult Clear Cell Sarcoma of Soft Parts|Adult Hepatocellular Carcinoma|Adult Rhabdomyosarcoma|Adult Soft Tissue Sarcoma|Childhood Alveolar Soft Part Sarcoma|Childhood Central Nervous System Neoplasm|Childhood Clear Cell Sarcoma of Soft Parts|Childhood Hepatocellular Carcinoma|Childhood Rhabdomyosarcoma|Childhood Soft Tissue Sarcoma|Childhood Solid Neoplasm|Ewing Sarcoma|Hepatoblastoma|Hepatocellular Carcinoma|Recurrent Adrenal Cortex Carcinoma|Recurrent Adult Hepatocellular Carcinoma|Recurrent Adult Soft Tissue Sarcoma|Recurrent Alveolar Soft Part Sarcoma|Recurrent Childhood Central Nervous System Neoplasm|Recurrent Childhood Hepatocellular Carcinoma|Recurrent Childhood Soft Tissue Sarcoma|Recurrent Ewing Sarcoma|Recurrent Hepatoblastoma|Recurrent Malignant Solid Neoplasm|Recurrent Renal Cell Carcinoma|Recurrent Rhabdomyosarcoma|Renal Cell Carcinoma|Thyroid Gland Medullary Carcinoma|Wilms Tumor Drug: Cabozantinib S-malate|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study National Cancer Institute (NCI) Phase 2 2017-07-01 2017-03-16
    NCT01811212 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 Drug: Cabozantinib S-malate|Other: Laboratory Biomarker Analysis National Cancer Institute (NCI)|Exelixis Phase 2 2013-05-01 2017-01-31
    NCT01835184 Recurrent Melanoma|Stage IIIA Melanoma|Stage IIIB Melanoma|Stage IIIC Melanoma|Stage IV Melanoma|Unspecified Adult Solid Tumor, Protocol Specific Drug: cabozantinib-s-malate|Drug: vemurafenib|Other: laboratory biomarker analysis|Other: pharmacological study National Cancer Institute (NCI) Phase 1 2013-05-01 2014-09-23
    NCT02243605 Metastatic Ewing Sarcoma|Metastatic Osteosarcoma|Recurrent Ewing Sarcoma|Recurrent Osteosarcoma|Stage III Osteosarcoma|Stage IV Osteosarcoma|Stage IVA Osteosarcoma|Stage IVB Osteosarcoma Drug: Cabozantinib S-malate|Other: Laboratory Biomarker Analysis National Cancer Institute (NCI) Phase 2 2014-12-01 2017-03-20
    NCT02315430 Fallopian Tube Clear Cell Adenocarcinoma|Ovarian Clear Cell Adenocarcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma Drug: Cabozantinib S-malate|Other: Laboratory Biomarker Analysis National Cancer Institute (NCI) Phase 2 2015-04-01 2017-03-23
    NCT01935934 Endometrial Adenosquamous Carcinoma|Endometrial Clear Cell Adenocarcinoma|Endometrial Mixed Adenocarcinoma|Endometrial Serous Adenocarcinoma|Metastatic Endometrioid Adenocarcinoma|Recurrent Uterine Corpus Carcinoma|Stage IV Uterine Corpus Cancer|Stage IVA Uterine Corpus Cancer|Stage IVB Uterine Corpus Cancer Drug: Cabozantinib S-malate|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study National Cancer Institute (NCI) Phase 2 2013-04-01 2017-03-20
    NCT01835158 Clear Cell Renal Cell Carcinoma|Metastatic Renal Cell Cancer|Stage III Renal Cell Cancer|Stage IV Renal Cell Cancer Drug: Cabozantinib S-malate|Other: Laboratory Biomarker Analysis|Drug: Sunitinib Malate National Cancer Institute (NCI) Phase 2 2013-07-01 2017-03-23
    NCT01866410 Recurrent Non-Small Cell Lung Carcinoma|Stage IV Non-Small Cell Lung Cancer Drug: Cabozantinib S-malate|Drug: Erlotinib Hydrochloride|Other: Laboratory Biomarker Analysis National Cancer Institute (NCI) Phase 2 2013-05-01 2016-12-26
    NCT02496208 Clear Cell Renal Cell Carcinoma|Renal Pelvis Urothelial Carcinoma|Stage III Bladder Adenocarcinoma|Stage III Bladder Squamous Cell Carcinoma|Stage III Bladder Urothelial Carcinoma|Stage III Renal Cell Cancer|Stage III Renal Pelvis Carcinoma|Stage III Ureter Cancer|Stage III Urethral Cancer|Stage IV Bladder Adenocarcinoma|Stage IV Bladder Squamous Cell Carcinoma|Stage IV Bladder Urothelial Carcinoma|Stage IV Renal Cell Cancer|Stage IV Renal Pelvis Carcinoma|Stage IV Ureter Cancer|Stage IV Urethral Cancer|Ureter Urothelial Carcinoma|Urethral Urothelial Carcinoma Drug: Cabozantinib S-malate|Biological: Ipilimumab|Other: Laboratory Biomarker Analysis|Biological: Nivolumab National Cancer Institute (NCI) Phase 1 2015-07-01 2017-03-20
    NCT01812668 Adenocarcinoma of the Prostate|Hormone-resistant Prostate Cancer|Recurrent Prostate Cancer|Stage IV Prostate Cancer Drug: cabozantinib-s-malate|Radiation: fluorine F 18 d-FMAU|Procedure: positron emission tomography|Other: pharmacological study|Other: laboratory biomarker analysis Barbara Ann Karmanos Cancer Institute|United States Department of Defense 2013-03-01 2016-02-08
    NCT01835145 Recurrent Uveal Melanoma|Stage III Uveal Melanoma|Stage IIIA Uveal Melanoma|Stage IIIB Uveal Melanoma|Stage IIIC Uveal Melanoma|Stage IV Uveal Melanoma Drug: Cabozantinib S-malate|Drug: Dacarbazine|Other: Laboratory Biomarker Analysis|Drug: Temozolomide National Cancer Institute (NCI)|Exelisis Phase 2 2013-07-01 2017-02-02
    NCT02761057 Recurrent Renal Cell Carcinoma|Stage III Renal Cell Cancer|Stage IV Renal Cell Cancer|Type 1 Papillary Renal Cell Carcinoma|Type 2 Papillary Renal Cell Carcinoma Drug: Cabozantinib S-malate|Drug: Crizotinib|Other: Laboratory Biomarker Analysis|Drug: Sunitinib Malate|Drug: Volitinib National Cancer Institute (NCI) Phase 2 2016-04-01 2017-03-23
    NCT01708954 Non-Small Cell Lung Cancer Drug: Cabozantinib|Drug: Erlotinib National Cancer Institute (NCI) Phase 2 2013-02-01 2016-11-30
    NCT01716715 Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma Drug: Cabozantinib S-malate|Other: Laboratory Biomarker Analysis|Drug: Paclitaxel National Cancer Institute (NCI) Phase 2 2012-11-01 2016-08-15
    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

    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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