Cabozantinib
- CAS No.
- 849217-68-1
- Chemical Name:
- Cabozantinib
- Synonyms
- XL184;Carbozantinib;N-(4-(6,7-diMethoxyquinolin-4-yloxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxaMide(CAS：849217-68-1);CS-6;XL-186;BMS907351;Cabotinib;Cabozantinib;Carbozanitinb;Phloroglucino
- CBNumber:
- CB72525898
- Molecular Formula:
- C28H24FN3O5
- Molecular Weight:
- 501.51
- MOL File:
- 849217-68-1.mol
- Modify Date:
- 2024/6/18 13:26:42
| Melting point | 212-215°C |
|---|---|
| Boiling point | 758.1±60.0 °C(Predicted) |
| Density | 1.396 |
| storage temp. | -20°C |
| solubility | Soluble in DMSO |
| form | White powder. |
| pka | 13.86±0.70(Predicted) |
| color | White |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
| InChIKey | ONIQOQHATWINJY-UHFFFAOYSA-N |
| SMILES | C1(C(NC2=CC=C(OC3C4C(N=CC=3)=CC(OC)=C(OC)C=4)C=C2)=O)(C(NC2=CC=C(F)C=C2)=O)CC1 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS05 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Danger | |||||||||
| Hazard statements | H315-H318 | |||||||||
| Precautionary statements | P264-P280-P302+P352-P321-P332+P313-P362-P280-P305+P351+P338-P310 | |||||||||
| NFPA 704 |
|
Cabozantinib Chemical Properties,Uses,Production
Description
Cabozantinib was approved inNovember 2012 for the treatment of patients with progressive, unresectable, locally advanced, or metastatic medullary thyroid cancer (MTC). Cabozantinib was granted orphan drug status by the FDA to facilitate development of newtreatment options for patients with MTC. It is a member of a class of tyrosine kinase inhibitors (TKIs) with nanomolar pan-inhibitory activity against VEGFR2, MET, and RET among others. Inhibition of the VEGF pathway has been shown preclinically to initially slow tumor growth, but rapid revascularization is followed by aggressive tumor growth. The MET pathway has been implicated in the development of VEGF resistance, so dual VEGF/MET activity is viewed as desirable. In addition, mutations in RET play a particular role in MTC, with 25% of the tumors inheriting a germlinemutation in the proto-oncogene, so multiple tyrosine kinase inhibition may be viewed as particularly beneficial for the treatment of MTC.
Uses
Cabozantinib (XL184, BMS-907351) is 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, respectively
Definition
ChEBI: A dicarboxylic acid diamide that is N-phenyl-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide in which the hydrogen at position 4 on the phenyl ring is substituted by a (6,7-dimethoxyquinolin-4-yl)oxy group. A multi-t rosine kinase inhibitor, used (as its malate salt) for the treatment of progressive, metastatic, medullary thyroid cancer.
General Description
Class:receptor tyrosine kinase; Treatment: MTC; RCC; HCC; Other name: XL-184, BMS-907351; Elimination half-life = 110 h; Protein binding > 99.7%
Clinical Use
Cabozantinib (PF-06463922; brand name Cabometyx; Exelixis, Alameda, CA) is an oral multikinase inhibitor with CNS penetration. It is FDA approved for use in medullary thyroid cancer and as a second-line agent in advanced renal cell carcinoma. In vitro studies found it to exhibit excellent activity against both the wild-type ROS1 fusion and the G2032R and G2026M mutations at concentrations less than 30?nmol/L—a dose much lower than what is clinically achievable [71, 91]. It has been found to inhibit CD74-ROS1-transformed Ba/F3 cells with more potency than entrectinib, brigatinib, lorlatinib [92], or foretinib [71].
target
RET/VEGFR
Cabozantinib Preparation Products And Raw materials
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| Basil Drugs AND Pharmaceuticals Pvt Ltd | +91-2249700250 +91-9619320820 | Mumbai, India | 108 | 58 | Inquiry |
| Vijaya Pharma And Life Science | +91-8939866271 +91-8939866271 | Tamil Nadu, India | 320 | 58 | Inquiry |
| Pharma Affiliates | 172-5066494 | Haryana, India | 6761 | 58 | Inquiry |
| SynZeal Research Pvt Ltd | +1 226-802-2078 | Gujarat, India | 6522 | 58 | Inquiry |
| Pharmaffiliates Analytics and Synthetics P. Ltd | +91-172-5066494 | Haryana, India | 6773 | 58 | Inquiry |
| Ujwala Pharmaceutical | 08048262407 | Pune, India | 3 | 58 | Inquiry |
| Malleshwar Speciality Medicals | 08046049021 | Karnataka, India | 1 | 58 | Inquiry |
| CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
| A.J Chemicals | 91-9810153283 | New Delhi, India | 6124 | 58 | Inquiry |
| Shandong Risen-Sun Pharmaceutical Co., Ltd | +86-15552509998 +86-15621883869 | China | 251 | 58 | Inquiry |
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