1. Protein Tyrosine Kinase/RTK
  2. VEGFR
    c-Met/HGFR
    c-Kit
    TAM Receptor
    FLT3

Cabozantinib (Synonyms: XL184; BMS-907351)

Cat. No.: HY-13016 Purity: 99.92%
Data Sheet SDS Handling Instructions

Cabozantinib is a potent multiple RTKs inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50 of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.

For research use only. We do not sell to patients.
Cabozantinib Chemical Structure

Cabozantinib Chemical Structure

CAS No. : 849217-68-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $66 In-stock
5 mg $60 In-stock
10 mg $75 In-stock
50 mg $99 In-stock
100 mg $145 In-stock
200 mg $245 In-stock
500 mg   Get quote  
1 g   Get quote  

* Please select Quantity before adding items.

Other Forms of Cabozantinib:

    Cabozantinib purchased from MCE. Usage Cited in: J Med Chem. 2016 Jan 14;59(1):358-73.

    Autophosphorylation of RET and its downstream signaling are blocked by 6i. The effect of 6i on autophosphorylation of RET in (A) RET-WT Ba/F3, (B) RET-S891A Ba/F3, (C) RET-V804L Ba/F3 and (D) RET-V804M Ba/F3. (A-D) Ba/F3 cells, stably transformed with the indicated constructs, are treated for 1 h with gradually increasing concentrations of 7a, Cabozantinib and 6i (0-10 μM) and then lysed. Protein extracts are immunoblotted with antibodies specific for the Y905 and Y1062 phosphorylated forms of R

    Cabozantinib purchased from MCE. Usage Cited in: J Med Chem. 2016 Jan 14;59(1):358-73.

    Autophosphorylation of RET and its downstream signaling are blocked by 6i. The effect of 6i on autophosphorylation of RET in (A) RET-WT Ba/F3, (B) RET-S891A Ba/F3, (C) RET-V804L Ba/F3 and (D) RET-V804M Ba/F3. (A-D) Ba/F3 cells, stably transformed with the indicated constructs, are treated for 1 h with gradually increasing concentrations of 7a, Cabozantinib and 6i (0-10 μM) and then lysed. Protein extracts are immunoblotted with antibodies specific for the Y905 and Y1062 phosphorylated forms of R

    Cabozantinib purchased from MCE. Usage Cited in: Mol Cancer Ther. 2017 Aug 3. pii: molcanther.0417.2017.

    Representative Western blots and densitometry show that cabozantinib reduces phosphorylation of Erk1/2 after 6 hours and reduces cyclin D1 and increases p27 protein levels after 24 hours of treatment (n=3-4).
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Cabozantinib is a potent multiple RTKs inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50 of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.

    IC50 & Target

    IC50: 0.035 nM (VEGFR2), 1.3 nM (c-Met), 4.6 nM (Kit), 7 nM (Axl), 11.3 nM (Flt3)[1]

    In Vitro

    Cabozantinib is a potent inhibitor of MET and VEGFR2 with IC50 values of 1.3 and 0.035 nM, respectively. MET-activating kinase domain mutations Y1248H, D1246N, or K1262R are also inhibited by Cabozantinib (IC50=3.8, 11.8, and 14.6 nM, respectively). Cabozantinib displays strong inhibition of several kinases that have also been implicated in tumor pathobiology, including KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). In cellular assays, Cabozantinib inhibits phosphorylation of MET and VEGFR2, as well as KIT, FLT3, and AXL with IC50 values of 7.8, 1.9, 5.0, 7.5, and 42 μM, respectively. The effect of Cabozantinib on proliferation is evaluated in a number of human tumor cell lines. SNU-5 and Hs746T cells harboring amplified MET are the most sensitive to Cabozantinib (IC50=19 and 9.9 nM, respectively); however, SNU-1 and SNU-16 cells lacking MET amplification are more resistant (IC50=5,223 and 1,149 nM, respectively). MDA-MB-231 and U87MG cells exhibit comparable levels of sensitivity to Cabozantinib (IC50=6,421 and 1,851 nM, respectively), whereas H441, H69, and PC3 cell lines are the least sensitive to Cabozantinib with IC50 values of 21,700, 20,200, and 10,800 nM, respectively. In addition, BaF3 cells expressing human FLT3-ITD, an activating mutation in acute myelogenous leukemia, are sensitive to Cabozantinib (IC50=15 nM) when compared with wild-type BaF3 cells (IC50=9,641 nM)[2].

    In Vivo

    Tumor vascularity decreases after Cabozantinib (XL184), with reductions ranging from 67% at 3 mg/kg to 83% at 30 mg/kg for 7 days[1]. In mouse models, Cabozantinib dramatically alters tumor pathology, resulting in decreased tumor and endothelial cell proliferation coupled with increased apoptosis and dose-dependent inhibition of tumor growth in breast, lung, and glioma tumor models. Importantly, treatment with Cabozantinib does not increase lung tumor burden in an experimental model of metastasis, which has been observed with inhibitors of VEGF signaling that do not target MET. On a body weight dosage basis, Cabozantinib plasma exposures range from 6- to 10-fold higher in rats than in mice, which accounts for lower doses inducing tumor growth inhibition/regression in rats than in mice. Subchronic administration of Cabozantinib is well tolerated in mice and rats with no signs of toxicity, as determined by stable and/or increasing body weights during the treatment period[2].

    Clinical Trial
    NCT Number Sponsor Condition Start Date Phase
    NCT01018745 Bristol-Myers Squibb Neoplasms January 2010 Phase 1
    NCT02101736 University of Alabama at Birmingham NF1|Neurofibromatosis|Plexiform Neurofibromas June 2014 Phase 2
    NCT01834651 Edwin Posadas, MD|Cedars-Sinai Medical Center Prostate Cancer April 30, 2013 Phase 2
    NCT01954745 Massachusetts General Hospital|Exelixis Bile Duct Cancer|Intrahepatic Cholangiocarcinoma|Cholangiocarcinoma of the Extrahepatic Bile Duct September 2013 Phase 2
    NCT02008383 John Strickler, M.D.|Exelixis|Duke University Colorectal Cancer January 2014 Phase 1
    NCT02036476 Dana-Farber Cancer Institute|Exelixis Merkel Cell Carcinoma|Skin Cancer January 2014 Phase 2
    NCT02302833 M.D. Anderson Cancer Center|Exelixis Neuroendocrine Tumors February 2015 Phase 2
    NCT01553656 Exelixis Solid Tumors|Cancer|NSCLC February 2011 Phase 1
    NCT01428219 University of Michigan Cancer Center|Exelixis Prostate Cancer Metastatic February 2012 Phase 2
    NCT01588821 Massachusetts General Hospital Lung Cancer|Solid Tumor (Not Breast or Prostate Cancers) June 2012 Phase 2
    NCT02885324 Indiana University Glioblastoma Multiforme|Anaplastic Astrocytoma|Malignant Brain Tumor|High Grade Glioma May 18, 2017 Phase 2
    NCT01738438 Dana-Farber Cancer Institute Breast Cancer February 2013 Phase 2
    NCT01582295 Massachusetts General Hospital Multiple Myeloma June 2012 Phase 1
    NCT01908426 Exelixis Hepatocellular Carcinoma August 2013 Phase 3
    NCT01709435 National Cancer Institute (NCI) Childhood Solid Neoplasm|Childhood Thyroid Gland Medullary Carcinoma|Recurrent Childhood Central Nervous System Neoplasm|Recurrent Malignant Solid Neoplasm|Recurrent Melanoma|Recurrent Thyroid Gland Carcinoma|Refractory Malignant Solid Neoplasm November 14, 2012 Phase 1
    NCT01961765 Massachusetts General Hospital|Exelixis Relapsed Acute Myeloid Leukemia|Refractory Acute Myeloid Leukemia November 2013 Phase 1
    NCT01493869 Exelixis Healthy|Hepatic Impairment September 2011 Phase 1
    NCT01663272 University of Michigan Cancer Center Pancreatic Cancer July 2012 Phase 1
    NCT01639508 Memorial Sloan Kettering Cancer Center|Exelixis Non-Small Cell Lung Cancer July 2012 Phase 2
    NCT03201250 Muhamed Baljevic, MD|M.D. Anderson Cancer Center|University of Nebraska Multiple Myeloma|Refractory Multiple Myeloma|Relapsed/Refractory Multiple Myeloma August 2017 Phase 1|Phase 2
    NCT01605227 Exelixis Prostate Cancer|Castration Resistant Prostate Cancer|Pain|Prostatic Neoplasms June 2012 Phase 3
    NCT01630590 M.D. Anderson Cancer Center|Exelixis|High Impact Clinical Research Support Program Prostate Cancer January 8, 2014 Phase 2
    NCT01865747 Exelixis Renal Cell Carcinoma June 2013 Phase 3
    NCT01866293 Memorial Sloan Kettering Cancer Center|Exelixis Relapsed or Refractory Multiple Myeloma May 28, 2013 Phase 1|Phase 2
    NCT01822522 National Cancer Institute (NCI) Advanced Malignant Solid Neoplasm|HIV Infection|Metastatic Malignant Solid Neoplasm|Recurrent Malignant Solid Neoplasm|Unresectable Solid Neoplasm June 21, 2013 Phase 1
    NCT01441947 Massachusetts General Hospital|Exelixis Breast Cancer October 2011 Phase 2
    NCT01703065 University of Washington|Prostate Cancer Foundation|National Cancer Institute (NCI) Adenocarcinoma of the Prostate|Castration-resistant Prostate Cancer|Recurrent Prostate Cancer|Stage III Prostate Cancer|Stage IV Prostate Cancer June 18, 2013
    NCT01466036 Massachusetts General Hospital Carcinoid Tumor|Pancreatic Neuroendocrine Tumor July 2012 Phase 2
    NCT03149822 University of Colorado, Denver|Merck Sharp & Dohme Corp. Metastatic Renal Cell Carcinoma August 2017 Phase 1|Phase 2
    NCT01811212 National Cancer Institute (NCI)|Exelixis 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 P May 8, 2013 Phase 2
    NCT02867592 National Cancer Institute (NCI) 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 Carci May 8, 2017 Phase 2
    NCT02132598 Liza Villaruz, MD|Exelixis|University of Pittsburgh Non Small Cell Lung Cancer (NSCLC)|Metastases to the Brain December 2015 Phase 2
    NCT02243605 National Cancer Institute (NCI) Metastatic Ewing Sarcoma|Metastatic Osteosarcoma|Recurrent Ewing Sarcoma|Recurrent Osteosarcoma|Stage III Osteosarcoma|Stage IV Osteosarcoma|Stage IVA Osteosarcoma|Stage IVB Osteosarcoma|Unresectable Ewing Sarcoma|Unresectable Osteosarcoma December 19, 2014 Phase 2
    NCT01761773 Exelixis Healthy|Renal Impairment December 2012 Phase 1
    NCT02315430 National Cancer Institute (NCI) Fallopian Tube Clear Cell Adenocarcinoma|Ovarian Clear Cell Adenocarcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma April 1, 2015 Phase 2
    NCT01708954 National Cancer Institute (NCI) Non-Small Cell Lung Cancer February 2013 Phase 2
    NCT01935934 National Cancer Institute (NCI) 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|Uterine Corpus Carcinosarcoma April 29, 2013 Phase 2
    NCT01835184 National Cancer Institute (NCI) Recurrent Melanoma|Stage IIIA Melanoma|Stage IIIB Melanoma|Stage IIIC Melanoma|Stage IV Melanoma|Unspecified Adult Solid Tumor, Protocol Specific May 2013 Phase 1
    NCT01995058 Exelixis Prostate Cancer|Castration Resistant Prostate Cancer|Prostatic Neoplasms December 2013 Phase 2
    NCT01347788 Massachusetts General Hospital Prostate Adenocarcinoma April 2011 Phase 1
    NCT01755195 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Refractory Soft Tissue Sarcomas December 7, 2012 Phase 2
    NCT01866410 National Cancer Institute (NCI) Recurrent Non-Small Cell Lung Carcinoma|Stage IV Non-Small Cell Lung Cancer AJCC v7 May 20, 2013 Phase 2
    NCT02260531 Dana-Farber Cancer Institute|Exelixis|Genentech, Inc. Breast Cancer|Brain Tumor - Metastatic October 2014 Phase 2
    NCT03170960 Exelixis Urothelial Carcinoma|Renal Cell Carcinoma June 2017 Phase 1|Phase 2
    NCT01896479 Exelixis Medullary Thyroid Cancer December 2014 Phase 4
    NCT01812668 Barbara Ann Karmanos Cancer Institute Adenocarcinoma of the Prostate|Hormone-resistant Prostate Cancer|Recurrent Prostate Cancer|Stage IV Prostate Cancer March 2013
    NCT01835158 National Cancer Institute (NCI) Clear Cell Renal Cell Carcinoma|Metastatic Renal Cell Cancer|Stage III Renal Cell Cancer|Stage IV Renal Cell Cancer July 8, 2013 Phase 2
    NCT01522443 Exelixis Prostate Cancer|Castration Resistant Prostate Cancer|Pain|Prostatic Neoplasms March 2012 Phase 3
    NCT01716715 National Cancer Institute (NCI) Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma November 2012 Phase 2
    NCT03200587 University of Utah|EMD Serono Renal Cell Carcinoma September 2017 Phase 1
    NCT02496208 National Cancer Institute (NCI) Clear Cell Renal Cell Carcinoma|Metastatic Malignant Neoplasm in the Bone|Metastatic Penile Carcinoma|Renal Pelvis Urothelial Carcinoma|Squamous Cell Carcinoma of the Penis|Stage III Bladder Adenocarcinoma|Stage III Bladder Squamous Cell Carcinoma|Stage III Bladder Urothelial Carcinoma|Stage III Penile Cancer|Stage III Renal Cell Cancer|Stage III Renal Pelvis Carcinoma|Stage III Ureter Cancer|Stage III Urethral Cancer|Stage IIIa Penile Cancer|Stage IIIb Penile Cancer|Stage IV Bladder Adenocarcin July 9, 2015 Phase 1
    NCT01599793 University of Chicago|NorthShore University HealthSystem Bone Metastases|Castrate-resistant Prostate Cancer|Recurrent Prostate Cancer|Stage IV Prostate Cancer May 2012 Phase 2
    NCT01683110 Exelixis Medullary Thyroid Cancer
    NCT01574937 Dana-Farber Cancer Institute Prostate Cancer September 2012 Phase 1
    NCT01835145 National Cancer Institute (NCI)|Exelisis Recurrent Uveal Melanoma|Stage III Uveal Melanoma|Stage IIIA Uveal Melanoma|Stage IIIB Uveal Melanoma|Stage IIIC Uveal Melanoma|Stage IV Uveal Melanoma July 31, 2013 Phase 2
    NCT01688999 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Urothelial Carcinoma|Urethral Neoplasms|Ureteral Neoplasms|Urinary Bladder Neoplasms|Kidney Neoplasms September 7, 2012 Phase 2
    NCT03213626 Bert Howard O'Neil|Exelixis|Indiana University Pancreatic Adenocarcinoma Metastatic August 1, 2017 Phase 2
    NCT02216578 European Organisation for Research and Treatment of Cancer - EORTC Metastatic Gastrointestinal Stromal Tumor February 2, 2017 Phase 2
    NCT02041260 Abramson Cancer Center of the University of Pennsylvania Differentiated Thyroid Cancer (DTC)|Poorly Differentiated Thyroid Cancer January 2014 Phase 2
    NCT01683994 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Prostatic Neoplasms September 6, 2012 Phase 1|Phase 2
    NCT02761057 National Cancer Institute (NCI) 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 April 5, 2016 Phase 2
    NCT01979393 European Organisation for Research and Treatment of Cancer - EORTC|Gynecologic Oncology Group|NHS Greater Glasgow and Clyde Uterine Sarcoma February 2015 Phase 2
    NCT03141177 Bristol-Myers Squibb Renal Cell Carcinoma July 10, 2017 Phase 3
    NCT02592356 M.D. Anderson Cancer Center Advanced Cancers|Endocrine Tumor November 2015
    NCT02293980 Peloton Therapeutics, Inc. ccRCC|RCC|Kidney Cancer|Clear Cell Renal Cell Carcinoma|Renal Cell Carcinoma November 2014 Phase 1
    NCT01658878 Bristol-Myers Squibb|Ono Pharmaceutical Co. Ltd Hepatocellular Carcinoma September 26, 2012 Phase 1|Phase 2
    NCT01018745 Bristol-Myers Squibb Neoplasms January 2010 Phase 1
    NCT02101736 University of Alabama at Birmingham NF1|Neurofibromatosis|Plexiform Neurofibromas June 2014 Phase 2
    NCT01834651 Edwin Posadas, MD|Cedars-Sinai Medical Center Prostate Cancer April 30, 2013 Phase 2
    NCT01954745 Massachusetts General Hospital|Exelixis Bile Duct Cancer|Intrahepatic Cholangiocarcinoma|Cholangiocarcinoma of the Extrahepatic Bile Duct September 2013 Phase 2
    NCT02008383 John Strickler, M.D.|Exelixis|Duke University Colorectal Cancer January 2014 Phase 1
    NCT02036476 Dana-Farber Cancer Institute|Exelixis Merkel Cell Carcinoma|Skin Cancer January 2014 Phase 2
    NCT02302833 M.D. Anderson Cancer Center|Exelixis Neuroendocrine Tumors February 2015 Phase 2
    NCT01553656 Exelixis Solid Tumors|Cancer|NSCLC February 2011 Phase 1
    NCT01428219 University of Michigan Cancer Center|Exelixis Prostate Cancer Metastatic February 2012 Phase 2
    NCT01588821 Massachusetts General Hospital Lung Cancer|Solid Tumor (Not Breast or Prostate Cancers) June 2012 Phase 2
    NCT02885324 Indiana University Glioblastoma Multiforme|Anaplastic Astrocytoma|Malignant Brain Tumor|High Grade Glioma May 18, 2017 Phase 2
    NCT01738438 Dana-Farber Cancer Institute Breast Cancer February 2013 Phase 2
    NCT01582295 Massachusetts General Hospital Multiple Myeloma June 2012 Phase 1
    NCT01908426 Exelixis Hepatocellular Carcinoma August 2013 Phase 3
    NCT01709435 National Cancer Institute (NCI) Childhood Solid Neoplasm|Childhood Thyroid Gland Medullary Carcinoma|Recurrent Childhood Central Nervous System Neoplasm|Recurrent Malignant Solid Neoplasm|Recurrent Melanoma|Recurrent Thyroid Gland Carcinoma|Refractory Malignant Solid Neoplasm November 14, 2012 Phase 1
    NCT01961765 Massachusetts General Hospital|Exelixis Relapsed Acute Myeloid Leukemia|Refractory Acute Myeloid Leukemia November 2013 Phase 1
    NCT01493869 Exelixis Healthy|Hepatic Impairment September 2011 Phase 1
    NCT01663272 University of Michigan Cancer Center Pancreatic Cancer July 2012 Phase 1
    NCT01639508 Memorial Sloan Kettering Cancer Center|Exelixis Non-Small Cell Lung Cancer July 2012 Phase 2
    NCT03201250 Muhamed Baljevic, MD|M.D. Anderson Cancer Center|University of Nebraska Multiple Myeloma|Refractory Multiple Myeloma|Relapsed/Refractory Multiple Myeloma August 2017 Phase 1|Phase 2
    NCT01605227 Exelixis Prostate Cancer|Castration Resistant Prostate Cancer|Pain|Prostatic Neoplasms June 2012 Phase 3
    NCT01630590 M.D. Anderson Cancer Center|Exelixis|High Impact Clinical Research Support Program Prostate Cancer January 8, 2014 Phase 2
    NCT01865747 Exelixis Renal Cell Carcinoma June 2013 Phase 3
    NCT01866293 Memorial Sloan Kettering Cancer Center|Exelixis Relapsed or Refractory Multiple Myeloma May 28, 2013 Phase 1|Phase 2
    NCT01822522 National Cancer Institute (NCI) Advanced Malignant Solid Neoplasm|HIV Infection|Metastatic Malignant Solid Neoplasm|Recurrent Malignant Solid Neoplasm|Unresectable Solid Neoplasm June 21, 2013 Phase 1
    NCT01441947 Massachusetts General Hospital|Exelixis Breast Cancer October 2011 Phase 2
    NCT01703065 University of Washington|Prostate Cancer Foundation|National Cancer Institute (NCI) Adenocarcinoma of the Prostate|Castration-resistant Prostate Cancer|Recurrent Prostate Cancer|Stage III Prostate Cancer|Stage IV Prostate Cancer June 18, 2013
    NCT01466036 Massachusetts General Hospital Carcinoid Tumor|Pancreatic Neuroendocrine Tumor July 2012 Phase 2
    NCT03149822 University of Colorado, Denver|Merck Sharp & Dohme Corp. Metastatic Renal Cell Carcinoma August 2017 Phase 1|Phase 2
    NCT01811212 National Cancer Institute (NCI)|Exelixis 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 P May 8, 2013 Phase 2
    NCT02867592 National Cancer Institute (NCI) 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 Carci May 8, 2017 Phase 2
    NCT02132598 Liza Villaruz, MD|Exelixis|University of Pittsburgh Non Small Cell Lung Cancer (NSCLC)|Metastases to the Brain December 2015 Phase 2
    NCT02243605 National Cancer Institute (NCI) Metastatic Ewing Sarcoma|Metastatic Osteosarcoma|Recurrent Ewing Sarcoma|Recurrent Osteosarcoma|Stage III Osteosarcoma|Stage IV Osteosarcoma|Stage IVA Osteosarcoma|Stage IVB Osteosarcoma|Unresectable Ewing Sarcoma|Unresectable Osteosarcoma December 19, 2014 Phase 2
    NCT01761773 Exelixis Healthy|Renal Impairment December 2012 Phase 1
    NCT02315430 National Cancer Institute (NCI) Fallopian Tube Clear Cell Adenocarcinoma|Ovarian Clear Cell Adenocarcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma April 1, 2015 Phase 2
    NCT01708954 National Cancer Institute (NCI) Non-Small Cell Lung Cancer February 2013 Phase 2
    NCT01935934 National Cancer Institute (NCI) 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|Uterine Corpus Carcinosarcoma April 29, 2013 Phase 2
    NCT01835184 National Cancer Institute (NCI) Recurrent Melanoma|Stage IIIA Melanoma|Stage IIIB Melanoma|Stage IIIC Melanoma|Stage IV Melanoma|Unspecified Adult Solid Tumor, Protocol Specific May 2013 Phase 1
    NCT01995058 Exelixis Prostate Cancer|Castration Resistant Prostate Cancer|Prostatic Neoplasms December 2013 Phase 2
    NCT01347788 Massachusetts General Hospital Prostate Adenocarcinoma April 2011 Phase 1
    NCT01755195 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Refractory Soft Tissue Sarcomas December 7, 2012 Phase 2
    NCT01866410 National Cancer Institute (NCI) Recurrent Non-Small Cell Lung Carcinoma|Stage IV Non-Small Cell Lung Cancer AJCC v7 May 20, 2013 Phase 2
    NCT02260531 Dana-Farber Cancer Institute|Exelixis|Genentech, Inc. Breast Cancer|Brain Tumor - Metastatic October 2014 Phase 2
    NCT03170960 Exelixis Urothelial Carcinoma|Renal Cell Carcinoma June 2017 Phase 1|Phase 2
    NCT01896479 Exelixis Medullary Thyroid Cancer December 2014 Phase 4
    NCT01812668 Barbara Ann Karmanos Cancer Institute Adenocarcinoma of the Prostate|Hormone-resistant Prostate Cancer|Recurrent Prostate Cancer|Stage IV Prostate Cancer March 2013
    NCT01835158 National Cancer Institute (NCI) Clear Cell Renal Cell Carcinoma|Metastatic Renal Cell Cancer|Stage III Renal Cell Cancer|Stage IV Renal Cell Cancer July 8, 2013 Phase 2
    NCT01522443 Exelixis Prostate Cancer|Castration Resistant Prostate Cancer|Pain|Prostatic Neoplasms March 2012 Phase 3
    NCT01716715 National Cancer Institute (NCI) Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma November 2012 Phase 2
    NCT03200587 University of Utah|EMD Serono Renal Cell Carcinoma September 2017 Phase 1
    NCT02496208 National Cancer Institute (NCI) Clear Cell Renal Cell Carcinoma|Metastatic Malignant Neoplasm in the Bone|Metastatic Penile Carcinoma|Renal Pelvis Urothelial Carcinoma|Squamous Cell Carcinoma of the Penis|Stage III Bladder Adenocarcinoma|Stage III Bladder Squamous Cell Carcinoma|Stage III Bladder Urothelial Carcinoma|Stage III Penile Cancer|Stage III Renal Cell Cancer|Stage III Renal Pelvis Carcinoma|Stage III Ureter Cancer|Stage III Urethral Cancer|Stage IIIa Penile Cancer|Stage IIIb Penile Cancer|Stage IV Bladder Adenocarcin July 9, 2015 Phase 1
    NCT01599793 University of Chicago|NorthShore University HealthSystem Bone Metastases|Castrate-resistant Prostate Cancer|Recurrent Prostate Cancer|Stage IV Prostate Cancer May 2012 Phase 2
    NCT01683110 Exelixis Medullary Thyroid Cancer
    NCT01574937 Dana-Farber Cancer Institute Prostate Cancer September 2012 Phase 1
    NCT01835145 National Cancer Institute (NCI)|Exelisis Recurrent Uveal Melanoma|Stage III Uveal Melanoma|Stage IIIA Uveal Melanoma|Stage IIIB Uveal Melanoma|Stage IIIC Uveal Melanoma|Stage IV Uveal Melanoma July 31, 2013 Phase 2
    NCT01688999 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Urothelial Carcinoma|Urethral Neoplasms|Ureteral Neoplasms|Urinary Bladder Neoplasms|Kidney Neoplasms September 7, 2012 Phase 2
    NCT03213626 Bert Howard O'Neil|Exelixis|Indiana University Pancreatic Adenocarcinoma Metastatic August 1, 2017 Phase 2
    NCT02216578 European Organisation for Research and Treatment of Cancer - EORTC Metastatic Gastrointestinal Stromal Tumor February 2, 2017 Phase 2
    NCT02041260 Abramson Cancer Center of the University of Pennsylvania Differentiated Thyroid Cancer (DTC)|Poorly Differentiated Thyroid Cancer January 2014 Phase 2
    NCT01683994 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Prostatic Neoplasms September 6, 2012 Phase 1|Phase 2
    NCT02761057 National Cancer Institute (NCI) 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 April 5, 2016 Phase 2
    NCT01979393 European Organisation for Research and Treatment of Cancer - EORTC|Gynecologic Oncology Group|NHS Greater Glasgow and Clyde Uterine Sarcoma February 2015 Phase 2
    NCT03141177 Bristol-Myers Squibb Renal Cell Carcinoma July 10, 2017 Phase 3
    NCT02592356 M.D. Anderson Cancer Center Advanced Cancers|Endocrine Tumor November 2015
    NCT02293980 Peloton Therapeutics, Inc. ccRCC|RCC|Kidney Cancer|Clear Cell Renal Cell Carcinoma|Renal Cell Carcinoma November 2014 Phase 1
    NCT01658878 Bristol-Myers Squibb|Ono Pharmaceutical Co. Ltd Hepatocellular Carcinoma September 26, 2012 Phase 1|Phase 2
    NCT01100619 Exelixis Papillary Thyroid Cancer|Follicular Thyroid Cancer|Huerthle Cell Thyroid Cancer|Renal Cell Carcinoma April 2010 Phase 1
    NCT00215605 Exelixis Lymphoma|Cancer|Thyroid Carcinoma September 2005 Phase 1
    NCT01068782 Exelixis Astrocytic Tumors April 2010 Phase 2
    NCT00704288 Exelixis Glioblastoma Multiforme May 2008 Phase 2
    NCT00940225 Exelixis Solid Tumors|Cancer August 2009 Phase 2
    NCT00596648 Exelixis Carcinoma, Non-Small-Cell Lung December 2007 Phase 1|Phase 2
    NCT00960492 Exelixis Glioblastoma|Giant Cell Glioblastoma|Gliosarcoma September 2009 Phase 1
    NCT00704730 Exelixis Thyroid Cancer June 2008 Phase 3
    View MoreCollapse
    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
    1 mM 1.9940 mL 9.9699 mL 19.9398 mL
    5 mM 0.3988 mL 1.9940 mL 3.9880 mL
    10 mM 0.1994 mL 0.9970 mL 1.9940 mL
    Kinase Assay
    [2]

    The inhibition profile of Cabozantinib against a broad panel of 270 human kinases is determined using luciferase-coupled chemiluminescence, 33P-phosphoryl transfer, or AlphaScreen technology. Recombinant human full-length, glutathione S-transferase tag, or histidine tag fusion proteins are used, and IC50 values are determined by measuring phosphorylation of peptide substrate poly(Glu, Tyr) at ATP concentrations at or below the Km for each respective kinase. The mechanism of kinase inhibition is evaluated using the AlphaScreen Assay by determining the IC50 values over a range of ATP concentrations[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [2]

    Cabozantinib is prepared in DMSO (10 mM) and serially diluted in the appropriate assay media[2].

    The effect of Cabozantinib on proliferation is evaluated in a number of human tumor cell lines, including SNU-5 and Hs746T cells harboring amplified MET, SNU-1 and SNU-16 cells, MDA-MB-231 and U87MG cells, H441, H69, and PC3 cell lines, and BaF3 cells. Cells are seeded in triplicate overnight in media containing 10% FBS. The next day, cells are treated with serial dilutions of Cabozantinib for 48 hours, followed by analysis of proliferation using Cell Proliferation ELISA, BrdUrd[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1][2]

    Cabozantinib (XL184) is suspended at a concentration of 5 mg/mL in sterile saline or water (Mice)[1].
    Cabozantinib is formulated in sterile saline/10 mM HCl or in water (Mice)[2].
    Cabozantinib is formulated in sterile saline/10 mM HCl or in water (Rat)[2].

    Mice[1]
    RIP-Tag2 mice in a C57BL/6 background are used as the tumor model. RIP-Tag2 mice are 10 weeks old at the onset of treatment unless otherwise indicated. Cabozantinib is suspended at a concentration of 5 mg/mL in sterile saline or water and administered by gavage daily for 7 days. Dose-dependent effects are studied in mice treated by gavage daily for 7 days: XL880 (1, 10, 20, 40 or 60 mg/kg), Cabozantinib (3, 10, 30, 40 or 60 mg/kg), or XL999 (25, 40, 50, 60 or 75 mg/kg). The time course of effects is studied in mice treated with XL880 (40 mg/kg) for 6 hr, 1, 4, 7 or 14 days. Effects of withdrawal are studied in mice treated with XL880 (40 mg/kg) for 7 days followed by no treatment for 0, 2, 7 or 14 days. Each group contain 4-6 mice.
    Mice[2]
    Female nu/nu mice are used. H441 cells (3×106) are implanted intradermally into the hind flank and when tumors reach approximately 150 mg, tumor weight is calculated using the formula: (tumor volume=length (mm)×width2(mm2)]/2, mice are randomized (n=5 per group) and orally administered a single 100 mg/kg dose of Cabozantinib or vehicle. Tumors are collected at the indicated time points. Pooled tumor lysates are subjected to immunoprecipitation with anti-MET and Western blotting with anti-phosphotyrosine MET. After blot stripping, total MET is quantitated as a loading control.
    Rat[2]
    On day 0 in female Wistar rats, C6 cells (5×106) are inoculated subcutaneously into the hind flank. When the tumors reach approximately 250 mg (3-4 days postimplantation), rats are randomized (n=8 per group) and treated orally once daily for 12 days with Cabozantinib or water vehicle. Cabozantinib administered via oral gavage at 2 mL/kg. Body weights are collected daily, and tumor weights are collected twice weekly. Percentage of tumor growth inhibition/regression values are expressed as follows: 1−[(mean treated tumor weight on the final day−mean tumor weight on day 0)/(mean vehicle tumor weight on the final day−mean tumor weight on day 0)]×100. Statistical analysis of Cabozantinib-treated tumors versus vehicle-treated tumors or versus predose tumors is done by one-way ANOVA with significance defined as P<0.05. Blood is collected 4 hours after the final dose, and plasma is prepared to determine Cabozantinib concentrations. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    501.51

    Formula

    C₂₈H₂₄FN₃O₅

    CAS No.

    849217-68-1

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 30 mg/mL

    Cabozantinib is prepared in 1.25% polyethylene glycol, 2.5% Tween-80, and 5% DMSO[3].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

    Purity: 99.92%

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number

     

    Organization name *

    Country *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Cabozantinib
    Cat. No.:
    HY-13016
    Quantity: