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Sitravatinib (MGCD516) - 96%, high purity , CAS No.1123837-84-2, Inhibitor of AXL receptor tyrosine kinase;Inhibitor of discoidin domain receptor tyrosine kinase 2;Inhibitor of EPH receptor A3;Inhibitor of fms related receptor tyrosine kinase 1;Inhibitor of fms related receptor tyrosine kinase 3;Inhibitor of fms relate

COA COA
In stock
Item Number
S414066
Grouped product items
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S414066-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$58.90
S414066-10mg
10mg
3
$88.90
S414066-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$167.90
S414066-50mg
50mg
3
$266.90
S414066-100mg
100mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$424.90
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VEGFR3 Selective Inhibitors

View related series
AXL receptor tyrosine kinase Inhibitor (18) c-Kit (81) Discoidin Domain Receptor (18) discoidin domain receptor tyrosine kinase 2 Inhibitor (9) EPH receptor A3 Inhibitor (4) FLT3 (103) fms related receptor tyrosine kinase 1 Inhibitor (33) fms related receptor tyrosine kinase 3 Inhibitor (60) fms related receptor tyrosine kinase 4 Inhibitor (30) kinase insert domain receptor Inhibitor (83) KIT proto-oncogene，receptor tyrosine kinase Inhibitor (51) MER proto-oncogene，tyrosine kinase Inhibitor (14) MET proto-oncogene，receptor tyrosine kinase Inhibitor (38) Neuronal Signaling (3320) neurotrophic receptor tyrosine kinase 1 Inhibitor (24) platelet derived growth factor receptor alpha Inhibitor (26) Protein Tyrosine Kinase/RTK (1314) Receptor Tyrosine Kinase (1260) Trk Receptor (42) VEGFR (187)

Basic Description

Synonyms DB15036 | CCG-270287 | EX-A2588 | DTXSID801100124 | 1,1-Cyclopropanedicarboxamide, N-(3-fluoro-4-((2-(5-(((2-methoxyethyl)amino)methyl)-2-pyridinyl)thieno(3,2-b)pyridin-7-yl)oxy)phenyl)-N'-(4-fluorophenyl)- | CS-5652 | Sitravatinib (USAN/INN) | BCP29099 |
Specifications & Purity Moligand™, ≥96%
Biochemical and Physiological Mechanisms Sitravatinib (MGCD516, MG-516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type INHIBITOR
Mechanism of action Inhibitor of AXL receptor tyrosine kinase;Inhibitor of discoidin domain receptor tyrosine kinase 2;Inhibitor of EPH receptor A3;Inhibitor of fms related receptor tyrosine kinase 1;Inhibitor of fms related receptor tyrosine kinase 3;Inhibitor of fms relate
Product Description

Information

Sitravatinib (MGCD516, MG-516) is a novel small molecule inhibitor targeting multipleRTKsinvolved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.


Targets

DDR2 (Cell-free assay); EPHA3 (Cell-free assay); Axl (Cell-free assay); Mer (Cell-free assay); VEGFR3 (FLT4) (Cell-free assay) 27977,0.5 nM; 1 nM; 1.5 nM; 2 nM; 2 nM


In vitro

MGCD516 (Sitravatinib), is an oral, potent small molecule inhibitor of a closely related spectrum of RTKs including RET, the split RTKs (VEGFR, PDGFR and KIT), TRK family, DDR2, MET and AXL. MGCD516 treatment resulted in significant blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects in vitro.


In vivo

Sitravatinib has demonstrated antitumor activity in nonclinical cancer models harboring genetic alterations of sitravatinib targets, including rearrangement of RET, NTRK, or CHR4q12 amplification. MGCD516 treatment of tumor xenografts in vivo resulted in significant suppression of tumor growth. Efficacy of MGCD516 was superior to imatinib and crizotinib, two other well-studied multi-kinase inhibitors with overlapping target specificities, both in vitro and in vivo.


Cell Research(from reference)

Cell lines：DDLS, LS141 and MPNST 

Concentrations：62.5, 125, 250, 500, 1000, 2000 nM/L 

Incubation Time：72 h 

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organic oxygen compounds
Class Organooxygen compounds
Subclass Ethers
Intermediate Tree Nodes Not available
Direct Parent Diarylethers
Alternative Parents Thienopyridines  Anilides  Phenoxy compounds  Phenol ethers  2,3,5-trisubstituted thiophenes  N-arylamides  Fluorobenzenes  Aralkylamines  Pyridines and derivatives  Aryl fluorides  Cyclopropanecarboxylic acids and derivatives  Heteroaromatic compounds  Secondary carboxylic acid amides  Amino acids and derivatives  Dialkylamines  Dialkyl ethers  Azacyclic compounds  Organofluorides  Organic oxides  Hydrocarbon derivatives  Carbonyl compounds  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Diaryl ether - Thienopyridine - Anilide - Phenoxy compound - Phenol ether - N-arylamide - 2,3,5-trisubstituted thiophene - Fluorobenzene - Halobenzene - Aralkylamine - Aryl fluoride - Aryl halide - Monocyclic benzene moiety - Cyclopropanecarboxylic acid or derivatives - Pyridine - Benzenoid - Heteroaromatic compound - Thiophene - Amino acid or derivatives - Secondary carboxylic acid amide - Carboxamide group - Organoheterocyclic compound - Azacycle - Secondary amine - Carboxylic acid derivative - Dialkyl ether - Secondary aliphatic amine - Organohalogen compound - Carbonyl group - Amine - Organofluoride - Organonitrogen compound - Organic nitrogen compound - Organic oxide - Hydrocarbon derivative - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as diarylethers. These are organic compounds containing the dialkyl ether functional group, with the formula ROR', where R and R' are aryl groups.
External Descriptors Not available

Associated Targets(Human)

DDR2 Tchem Discoidin domain-containing receptor 2 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
EPHA3 Tchem Ephrin type-A receptor 3 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FLT4 Tclin Vascular endothelial growth factor receptor 3 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
MET Tclin Hepatocyte growth factor receptor (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
MERTK Tchem Tyrosine-protein kinase Mer (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PDGFRA Tclin Platelet-derived growth factor receptor alpha (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FLT1 Tclin Vascular endothelial growth factor receptor 1 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
KDR Tclin Vascular endothelial growth factor receptor 2 (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
AXL Tchem Tyrosine-protein kinase receptor UFO (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
KIT Tclin Mast/stem cell growth factor receptor Kit (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
NTRK2 Tclin BDNF/NT-3 growth factors receptor (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
NTRK1 Tclin High affinity nerve growth factor receptor (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
KIT Tclin Stem cell growth factor receptor (10667 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KDR Tclin Vascular endothelial growth factor receptor 2 (20924 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MET Tclin Hepatocyte growth factor receptor (10718 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NTRK1 Tclin Nerve growth factor receptor Trk-A (7922 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
FLT3 Tclin Tyrosine-protein kinase receptor FLT3 (13481 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HepG2 (196354 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AXL Tchem Tyrosine-protein kinase receptor UFO (3469 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NTRK2 Tclin Neurotrophic tyrosine kinase receptor type 2 (3279 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

Pubchem Sid 504770022
Pubchem Sid Url https://pubchem.ncbi.nlm.nih.gov/substance/504770022
IUPAC Name 1-N'-[3-fluoro-4-[2-[5-[(2-methoxyethylamino)methyl]pyridin-2-yl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
INCHI InChI=1S/C33H29F2N5O4S/c1-43-15-14-36-18-20-2-8-25(38-19-20)29-17-26-30(45-29)28(10-13-37-26)44-27-9-7-23(16-24(27)35)40-32(42)33(11-12-33)31(41)39-22-5-3-21(34)4-6-22/h2-10,13,16-17,19,36H,11-12,14-15,18H2,1H3,(H,39,41)(H,40,42)
InChIKey WLAVZAAODLTUSW-UHFFFAOYSA-N
Smiles COCCNCC1=CN=C(C=C1)C2=CC3=NC=CC(=C3S2)OC4=C(C=C(C=C4)NC(=O)C5(CC5)C(=O)NC6=CC=C(C=C6)F)F
Isomeric SMILES COCCNCC1=CN=C(C=C1)C2=CC3=NC=CC(=C3S2)OC4=C(C=C(C=C4)NC(=O)C5(CC5)C(=O)NC6=CC=C(C=C6)F)F
PubChem CID 25212148
Molecular Weight 629.68

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

2 results found

Lot Number Certificate Type Date Item
G2209403 Certificate of Analysis Apr 03, 2025 S414066
G2209388 Certificate of Analysis Apr 03, 2025 S414066

Chemical and Physical Properties

Solubility Solubility (25°C) In vitro DMSO: 100 mg/mL (158.81 mM); Ethanol: 100 mg/mL (158.81 mM); Water: Insoluble;
Molecular Weight 629.700 g/mol
XLogP3 5.200
Hydrogen Bond Donor Count 3
Hydrogen Bond Acceptor Count 10
Rotatable Bond Count 12
Exact Mass 629.191 Da
Monoisotopic Mass 629.191 Da
Topological Polar Surface Area 143.000 Ų
Heavy Atom Count 45
Formal Charge 0
Complexity 1000.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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