Home Protein Tyrosine Kinase CSF-1R inhibitor - VEGFR inhibitor - FGFR inhibitor Sulfatinib For research use only.

Sulfatinib

Synonyms: HMPL-012, Surufatinib

Sulfatinib is a potent and highly selective tyrosine kinase inhibitor against VEGFR1, VEGFR2, VEGFR3, FGFR1 and CSF1R with IC50 of 2 nM, 24 nM, 1 nM, 15 nM and 4 nM, respectively. Sulfatinib shows encouraging antitumor activity and manageable toxicities in patients with advanced NETs.

Sulfatinib Chemical Structure

Sulfatinib Chemical Structure

CAS No. 1308672-74-3

Purity & Quality Control

Sulfatinib Related Products

Signaling Pathway

CSF-1R Signaling Pathways

CSF-1R Signaling Pathway

Biological Activity

Description Sulfatinib is a potent and highly selective tyrosine kinase inhibitor against VEGFR1, VEGFR2, VEGFR3, FGFR1 and CSF1R with IC50 of 2 nM, 24 nM, 1 nM, 15 nM and 4 nM, respectively. Sulfatinib shows encouraging antitumor activity and manageable toxicities in patients with advanced NETs.
Targets
VEGFR3 [1]
(Cell-free assay)		 VEGFR1 [1]
(Cell-free assay)		 CSF1R [1]
(Cell-free assay)		 FGFR1 [1]
(Cell-free assay)		 VEGFR2 [1]
(Cell-free assay)
1 nM 2 nM 4 nM 15 nM 24 nM
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03627520 Completed
Healthy
Hutchison Medipharma Limited|Hutchmed
 April 2 2018 Early Phase 1
NCT03483259 Completed
Relative Bioavailability
Hutchison Medipharma Limited|Hutchmed
 April 2 2018 Phase 1
NCT02320409 Completed
Healthy
Hutchison Medipharma Limited|Hutchmed
 December 2014 Phase 1
NCT02133157 Completed
Tumor
Hutchison Medipharma Limited|Hutchmed
 April 2010 Phase 1

Chemical Information & Solubility

Molecular Weight 480.58 Formula

C24H28N6O3S
CAS No. 1308672-74-3 SDF --
Smiles CC1=CC2=C(N1)C=CC(=C2)OC3=NC(=NC=C3)NC4=CC=CC(=C4)CS(=O)(=O)NCCN(C)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 96 mg/mL ( (199.75 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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