Available from stock

Cabozantinib

SKU: C0755

Category: Building Blocks, Intermediates, Reagents

Synonyms: BMS-907351 , XL184; 849217-68-1
CAS-Number: C₂₈H₂₄FN₃O₅
Molecular Formula: 501.5
Molecular Weight

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

Product Data
Handling
Safety Information
Details

Specifications

Purity: ≥98% (HPLC)
Appearance: White to off-white solid
Identity: 1H-NMR

Properties

Solvents: DMSO (20 mg/ml). Slightly ethanol.

Documentation

Safety Data Sheet (SDS): CDX C0755 MSDS.pdf

Shipping: AMBIENT
Short Term Storage: +4°C
Long Term Storage: -20°C
Handling Advice: Protect from light and moisture.
Use / Stability: Stable for at least 2 years after receipt when stored at -20°C.

Transportation: Not dangerous goods

Description: Cabozantinib is a potent multi-targeted receptor tyrosine kinase (RTK) inhibitor of endothelial growth factor receptor 2 (VEGFR2) (IC50=0.035nM), the hepatocyte growth factor receptor c-Met (IC50=1.3nM), AXL (IC50=7nM), fms like tyrosine kinase 3 (FLT3) (IC50=11.3nM), mast/stem cell growth factor (KIT) (IC50=4.6nM), RET (IC50=5.2nM), tyrosine-protein kinase receptor (TIE-2) (IC50=14.3nM) and RON (IC50=124nM). Cabozantinib reduces cell proliferation and vascular density. It also induces apoptosis and intratumoral hypoxia. Cabozantinib exhibits dose-related tumor growth inhibition, tumor regression, angiogenesis and/or metastasis inhibition in a broad range of preclinical tumor models. The anticancer compound cabozantinib has undergone clinical trial in a broad number of cancers, including thyroid carcinoma, prostate cancer, ovarian cancer, melanoma, breast cancer, non-small cell lung cancer, hepatocellular cancer, renal cell carcinoma and glioblastoma.
Smiles: O=C(NC1=CC=C(OC2=C3C=C(C(OC)=CC3=NC=C2)OC)C=C1)C4(C(NC5=CC=C(C=C5)F)=O)CC4
InChi Key: ONIQOQHATWINJY-UHFFFAOYSA-N
References: (1) Y. Zhang, et al., IDrugs 13, 112 (2010) , (2) R. Kurzrock, et al., J. Clin. Oncol. 29, 2660 (2011) , (3) F.M. Yakes, et al., Mol. Canc. Ther. 10, 2298 (2011) , (4) S. Roy, et al., Anticancer Agents Med. Chem. 15, 37 (2015) (Review) , (5) N.M. Tannir, et al., Curr. Oncol. Rep. 19, 14 (2017) (Review) , (6) C. Grullich, Recent Res. Cancer Res. 211, 67 (2018) (Review) , (7) J.N. Markowitz & K.M. Fancher,, Pharmacotherapy 38, 357 (2018) (Review) , (8) A. Desai & E.J. Small, Future Oncol. 15, 2337 (2019) (Review) , (9) J. Trojan, Drugs 80, 1203 (2020) (Review)
InChi: InChI=1S/C28H24FN3O5/c1-35-24-15-21-22(16-25(24)36-2)30-14-11-23(21)37-20-9-7-19(8-10-20)32-27(34)28(12-13-28)26(33)31-18-5-3-17(29)4-6-18/h3-11,14-16H,12-13H2,1-2H3,(H,31,33)(H,32,34)

Cabozantinib is a potent multi-targeted receptor tyrosine kinase (RTK) inhibitor of endothelial growth factor receptor 2 (VEGFR2) (IC50=0.035nM), the hepatocyte growth factor receptor c-Met (IC50=1.3nM), AXL (IC50=7nM), fms like tyrosine kinase 3 (FLT3) (IC50=11.3nM), mast/stem cell growth factor (KIT) (IC50=4.6nM), RET (IC50=5.2nM), tyrosine-protein kinase receptor (TIE-2) (IC50=14.3nM) and RON (IC50=124nM). Cabozantinib reduces cell proliferation and vascular density. It also induces apoptosis and intratumoral hypoxia. Cabozantinib exhibits dose-related tumor growth inhibition, tumor regression, angiogenesis and/or metastasis inhibition in a broad range of preclinical tumor models. The anticancer compound cabozantinib has undergone clinical trial in a broad number of cancers, including thyroid carcinoma, prostate cancer, ovarian cancer, melanoma, breast cancer, non-small cell lung cancer, hepatocellular cancer, renal cell carcinoma and glioblastoma.

SKU: C0755 Category: Building Blocks, Intermediates, Reagents

Additional information

Additional information

Synonyms	BMS-907351, XL184
Purity	≥98% (HPLC)
Appearance	White to off-white solid
CAS-Number	849217-68-1
Molecular Formula	C28H24FN3O5
Molecular Weight	501.5
Identity	1H-NMR
Solvents	DMSO (20 mg/ml). Slightly ethanol.
Smiles	O=C(NC1=CC=C(OC2=C3C=C(C(OC)=CC3=NC=C2)OC)C=C1)C4(C(NC5=CC=C(C=C5)F)=O)CC4
InChi Key	ONIQOQHATWINJY-UHFFFAOYSA-N
Shipping	AMBIENT
Short Term Storage	+4°C
Long Term Storage	-20°C
Handling Advice	Protect from light and moisture.
Use / Stability	Stable for at least 2 years after receipt when stored at -20°C.
Transportation	Not dangerous goods
References	(1) Y. Zhang, et al., IDrugs 13, 112 (2010), (2) R. Kurzrock, et al., J. Clin. Oncol. 29, 2660 (2011), (3) F.M. Yakes, et al., Mol. Canc. Ther. 10, 2298 (2011), (4) S. Roy, et al., Anticancer Agents Med. Chem. 15, 37 (2015) (Review), (5) N.M. Tannir, et al., Curr. Oncol. Rep. 19, 14 (2017) (Review), (6) C. Grullich, Recent Res. Cancer Res. 211, 67 (2018) (Review), (7) J.N. Markowitz & K.M. Fancher,, Pharmacotherapy 38, 357 (2018) (Review), (8) A. Desai & E.J. Small, Future Oncol. 15, 2337 (2019) (Review), (9) J. Trojan, Drugs 80, 1203 (2020) (Review)
InChi	InChI=1S/C28H24FN3O5/c1-35-24-15-21-22(16-25(24)36-2)30-14-11-23(21)37-20-9-7-19(8-10-20)32-27(34)28(12-13-28)26(33)31-18-5-3-17(29)4-6-18/h3-11,14-16H,12-13H2,1-2H3,(H,31,33)(H,32,34)
Quantity	10 mg, 50 mg, Bulk