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Cabozantinib S-malate

Cabozantinib S-malate structure

CAS No:
1140909-48-3
Formula:
C28H24FN3O5.C4H6O5
Chemical Name:
Cabozantinib S-malate
Synonyms:
Butanedioic acid,2-hydroxy-,(2S)-,compd. with N-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl]-N′-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide (1:1);XL 184;Cabozantinib S-malate;Cometriq;(2S)-2-Hydroxybutanedioic acid compd. with N-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl]-N′-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide (1:1);942407-59-2
Categories:
Biochemical Engineering > Inhibitors

Description

Off-White SolidChEBI: A malate salt that is the mono-(S)-malate salt of cabozantinib. A multi-tyrosine kinase inhibitor, used for the treatment of progressive, metastatic, medullary thyroid cancer.

Cabozantinib malate is a malate salt that is the mono-(S)-malate salt of cabozantinib. A multi-tyrosine kinase inhibitor, used for the treatment of progressive, metastatic, medullary thyroid cancer. It has a role as a tyrosine kinase inhibitor, an antineoplastic agent and a prodrug. It contains a cabozantinib.|Cabozantinib S-malate is the s-malate salt form of cabozantinib, an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. Cabozantinib strongly binds to and inhibits several RTKs, which are often overexpressed in a variety of cancer cell types, including hepatocyte growth factor receptor (MET), RET (rearranged during transfection), vascular endothelial growth factor receptor types 1 (VEGFR-1), 2 (VEGFR-2), and 3 (VEGFR-3), mast/stem cell growth factor (KIT), FMS-like tyrosine kinase 3 (FLT-3), TIE-2 (TEK tyrosine kinase, endothelial), tropomyosin-related kinase B (TRKB) and AXL. This may result in an inhibition of both tumor growth and angiogenesis, and eventually lead to tumor regression.

Cabozantinib S-malate Basic Attributes

Molecular Weight：

635.5931032

Exact Mass：

635.191522

UNII：

DR7ST46X58

NCI Thesaurus Code：

C97938

ATC Code：

L01XE26

Characteristics

PSA：

194

XLogP3：

4.59340

Safety Information

GHS Classification：

|Danger|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P201, P202, P260, P261, P264, P270, P271, P280, P281, P301+P312, P302+P352, P304+P340, P305+P351+P338, P308+P313, P312, P314, P321, P330, P332+P313, P337+P313, P362, P403+P233, P405, and P501|Aggregated GHS information provided by 51 companies from 5 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Drug Indication：

Renal Cell Carcinoma (RCC)Cabometyx is indicated as monotherapy for the treatment of advanced renal cell carcinoma (RCC):in treatment-naïve adults with intermediate or poor risk,in adults following prior vascular endothelial growth factor (VEGF)-targeted therapy.Cabometyx, in combination with nivolumab, is indicated for the first-line treatment of advanced renal cell carcinoma in adults.Hepatocellular Carcinoma (HCC)Cabometyx is indicated as monotherapy for the treatment of hepatocellular carcinoma (HCC) in adults who have previously been treated with sorafenib.|Drug: Cabozantinib-s-malate

MeSH Entry Terms：

BMS 907351

Cabozantinib S-malate Use and Manufacturing

Uses

Cabozantinib is a small molecule C-Met modulator. Cabozantinib acts as a potent multitargeted VEGFR2, Met, FLT3, Tie2, Kit and Ret inhibitor with IC50 of 0.035, 1.8, 14.4, 14.3 and 4.6 nM for VEGFR2, Met, FLT3, Tie2 and Kit, respectively. Cabozantinib shows dose-dependent inhibition of tumor growth and tumor regression, associated with disruption of the tumor vasculature and extensive tumor cell a poptosis. XL184 (Cabozantinib, BMS-907351) is a potent multitargeted VEGFR2, Met, FLT3, Tie2, K

Use Classification：

Human drugs -> Cabometyx -> EMA Drug Category|Antineoplastic agents -> Human pharmacotherapeutic group|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:635.6
Hydrogen Bond Donor Count:5
Hydrogen Bond Acceptor Count:12
Rotatable Bond Count:11
Exact Mass:635.19152232
Monoisotopic Mass:635.19152232
Topological Polar Surface Area:194
Heavy Atom Count:46
Complexity:924
Defined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

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