what is Cabozantinib Powder?
Cabozantinib is a novel molecular targeted drug developed by Exelixis Biopharmaceutical Company in the United States. On November 29, 2012, the US Food and Drug Administration (FDA) approved cabozantinib for the treatment of unresectable malignant locally advanced or metastatic medullary thyroid cancer.Cabozantinib Powder is in a class of medications called kinase inhibitors.It works by blocking the action of an abnormal protein that signals cancer cells to multiply. This helps slow or stop the spread of cancer cells.
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Product name |
Cabozantinib |
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CAS |
849217-68-1 |
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Molecular formula |
C28H24FN3O5 |
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Molecular weight |
501.51 |
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EINECS Number |
692-846-8 |
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Storage condition |
-20°C Freezer |
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Appearance |
white powder |
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melting point |
212-215°C | |
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Solubility |
Dissolved in dimethyl sulfoxide |
Does Cabozantinib Powder have biological activity?
Cabozantinib Powder (XL184, BMS-907351) is an effective VEGFR2 inhibitor with an IC50 of 0.035nM in cell-free assays. It also effectively inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 values of 1.3nM, 4nM, 4.6nM, 12nM/11.3nM/6nM, 14.3nM, and 7nM, respectively. Cabozantinib can induce PUMA dependent apoptosis in colon cancer cells through the AKT/GSK-3 β/NF - κ B signaling pathway.
How does Cabozantinib Powder work?
Cabozantinib Powder works in 2 ways:
stops cancers from growing their own blood vessels which supplies it with food and oxygen to grow
blocks the messages that tells the cancer cells to grow
In vitro biochemical and/or cytological analysis showed that cabozantinib inhibits RET, human hepatocyte growth factor receptor (MET), vascular endothelial growth factor receptor 1 (VEGFR-1), VEGFR-2, VEGFR-3, stem cell growth factor receptor (KIT), tyrosine kinase receptor (TRKB), FMS like chemical book tyrosine kinase 3 (FLT-3), AXL, and human growth factor like domain tyrosine kinase 2 (HGF-2). Without immunoglobulin like and EGF like domains2 (TIE-2) The tyrosine kinase activity of these kinase receptors plays an important role in the growth process of both normal cells and tumor cells. Abnormal expression of these receptors plays an important role in the occurrence and development of various tumors, including inhibiting tumor cell apoptosis, participating in pathological processes such as tumor angiogenesis and invasion. Cabozantinib exerts anti-tumor effects by inhibiting the activity of the aforementioned kinases, killing tumor cells, reducing metastasis, and inhibiting tumor angiogenesis
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Product Specification
| Analysis tests | Standard | Result |
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Appearance |
white powder |
Conforms |
| Identification | H-NMR | Conforms |
| Individual impurity | ≤0.5% | 0.23% |
| Total impurity | ≤1.0% | 0.33% |
| Purity | 98.0%-100% | 99.5% |
Conclusion：Conform with specification and qualified.
Does Cabozantinib Powder have any Adverse effects?
In clinical trials, common adverse reactions caused by cabozantinib include diarrhea, stomatitis, Palmar plantar erythropathy syndrome (PPES), weight loss, loss of appetite, nausea, fatigue, oral pain, color changes, taste disorders, high blood pressure, abdominal pain, and constipation. The most common laboratory abnormalities (>25%) are an increase in aspartate aminotransferase and alanine aminotransferase, a decrease in lymphocytes, an increase in alkaline phosphatase, hypocalcemia, neutropenia, thrombocytopenia, hypophosphatemia, and hyperbilirubinemia. After the first dose of cabozantinib treatment, 57% of patients showed an increase in thyroid stimulating hormone (TSH) levels, which was 19% higher compared to patients receiving placebo.
What are the relevant studies of Cabozantinib?
In vitro research
XL184 is a small molecule inhibitor of various receptor tyrosine kinases, particularly inhibiting c-Met and VEGFR2. XL-184 also effectively acts on Ret, Kit,FLT1,FLT3,FLT4,Tie2, The IC50 values for AXL are 4nM, 4.6nM, 12nM, 11.3nM, 6nM, 14.3nM, and 7nM, respectively. XL184 weakly inhibits RON and PDGFR - β with IC50 values of 124nM and 234nM, respectively, while it has almost no inhibitory activity on FGFR1 with an IC50 value of 5.294 μ M. Treatment of MPNST cells with XL184 at low concentrations (0.1-0.5 μ M) significantly inhibited constitutive and inducible Met phosphorylation and downstream signaling, as well as HGF induced MPNST cell migration and invasion.Cabozantinib Powder acts on cytokine stimulated human umbilical vein endothelial cells (HUVECs) and significantly inhibits Met and VEGFR2 phosphorylation. Although XL184 cannot inhibit the growth of MPNST cells at a concentration of 0.1 μ M, it can significantly inhibit the growth of MPNST cells . However, at a concentration of 5-10 μ M, it can significantly inhibit the growth of MPNST cells.
In vivo research
XL184 treated RIP-Tag2 mice carrying spontaneous pancreatic islet cell tumors at a dose of 30mg/kg disrupted 83% of tumor blood vessels, reduced pericytes and empty basement membrane sleeves, caused widespread intratumoral hypoxia and extensive tumor cell apoptosis, and delayed tumor blood vessel regrowth after discontinuation. Compared with XL999,Cabozantinib significantly inhibited VEGFR rather than c-Met, resulting in a 43% decrease in blood vessels, indicating that inhibition of VEGFR also inhibited other functionally related receptor tyrosine kinases (RTK) that amplify and inhibit angiogenesis. XL184 also reduces the invasion and metastasis of primary tumors. XL184 treatment of SCID mice at a dose of 30mg/kg per day significantly abolished the growth and metastasis of human MPNST transplanted tumors. Cabozantinib can inhibit the growth of breast cancer and lung cancer glioma models in a dose-dependent manner, reduce the proliferation of tumor and endothelial cells, and promote apoptosis. XL184 treated mice carrying MDA-MB-231 tumors and rats carrying C6 tumors separately at doses of 100mg/kg and 10mg/kg, respectively, to continuously inhibit tumor growth.
How and where to buy Cabozantinib Powder wholesale?
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We ensure the quality of our products through independent experimental testing, and every customer is our VIP.
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A variety of shipping methods for you to choose
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Transportation Time |
Shipping method |
Cargo weight requirements |
Advantage |
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3-7 days |
DHL, Germany DHL, Germany DPD, |
Suitable for under 50kg. |
We have warehouses in Germany and California, USA, |
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7-15 days |
By Air |
Suitable for more than 50kg. |
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15-60 days |
By Sea |
Suitable for more than 500kg. |
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Note: The product is for research use only and is not intended for diagnosis, treatment, disease prevention, etc.
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