Sitravatinib (MGCD516) - Moligand™, 10mM in DMSO , 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, 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

CAS: 1123837-84-2 Cat. No.: S408996 Formula: C₃₃H₂₉F₂N₅O₄S Peso molecolare: 629.68 Numero EC: 863-087-1 PubChem CID: 25212148

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

MG-516 | 1,​1-​Cyclopropanedicarbox​amide, N-​[3-​fluoro-​4-​[[2-​[5-​[[(2-​methoxyethyl)​amino]​methyl]​-​2-​pyridinyl]​thieno[3,​2-​b]​pyridin-​7-​yl]​oxy]​phenyl]​-​N'-​(4-​fluorophenyl)​-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

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.
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 Data

cell lines：Primary human keratinocytes

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

Incubation Time：72 h

Powder Purity:≥96%

Specifications

Sinonimi

MG-516 | 1,​1-​Cyclopropanedicarbox​amide, N-​[3-​fluoro-​4-​[[2-​[5-​[[(2-​methoxyethyl)​amino]​methyl]​-​2-​pyridinyl]​thieno[3,​2-​b]​pyridin-​7-​yl]​oxy]​phenyl]​-​N'-​(4-​fluorophenyl)​-

Specifiche e purezza

Moligand™, 10mM in DMSO

Meccanismi biochimici e fisiologici

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.

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Grado

Moligand™

Tipo di azione

INHIBITOR

Meccanismo d'azione

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

Nomi e identificatori

Isomeri 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

Peso molecolare

629.68

Obiettivi associati (umani)

DDR2 Tchem Discoidin domain-containing receptor 2 (1 Activities)

Discover Target: DDR2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

EPHA3 Tchem Ephrin type-A receptor 3 (1 Activities)

Discover Target: EPHA3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FLT4 Tclin Vascular endothelial growth factor receptor 3 (1 Activities)

Discover Target: FLT4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 (1 Activities)

Discover Target: FLT3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MET Tclin Hepatocyte growth factor receptor (1 Activities)

Discover Target: MET

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MERTK Tchem Tyrosine-protein kinase Mer (1 Activities)

Discover Target: MERTK

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDGFRA Tclin Platelet-derived growth factor receptor alpha (1 Activities)

Discover Target: PDGFRA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FLT1 Tclin Vascular endothelial growth factor receptor 1 (1 Activities)

Discover Target: FLT1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KDR Tclin Vascular endothelial growth factor receptor 2 (1 Activities)

Discover Target: KDR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AXL Tchem Tyrosine-protein kinase receptor UFO (1 Activities)

Discover Target: AXL

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KIT Tclin Mast/stem cell growth factor receptor Kit (1 Activities)

Discover Target: KIT

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NTRK2 Tclin BDNF/NT-3 growth factors receptor (0 Activities)

Discover Target: NTRK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NTRK1 Tclin High affinity nerve growth factor receptor (1 Activities)

Discover Target: NTRK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Proprietà chimiche e fisiche

• Solubilità: Solubility (25°C) In vitro DMSO: 54 mg/mL (199.82 mM); Ethanol: 1 mg/mL (3.7 mM); Water: Insoluble

Domande frequenti

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1123837-84-2, the molecular formula is C33H29F2N5O4S, and the molecular weight is 629.68 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.