Sulfatinib

Catalog No.S0487 Synonyms: HMPL-012, Sufatinib, Surfatinib, Surufatinib

For research use only.

Sulfatinib (HMPL-012, Sufatinib, Surfatinib, Surufatinib) 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

CAS No. 1308672-74-3

Purity & Quality Control

Choose Selective CSF-1R Inhibitors

Biological Activity

Description Sulfatinib (HMPL-012, Sufatinib, Surfatinib, Surufatinib) 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

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 480.58
Formula

C24H28N6O3S

CAS No. 1308672-74-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC2=C(N1)C=CC(=C2)OC3=NC(=NC=C3)NC4=CC=CC(=C4)CS(=O)(=O)NCCN(C)C

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

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03627520 Completed Drug: [14C]Sulfatinib Healthy Hutchison Medipharma Limited April 2 2018 Early Phase 1
NCT03483259 Completed Drug: Sulfatinib T capsule|Drug: Sulfatinib R capsule Relative Bioavailability Hutchison Medipharma Limited April 2 2018 Phase 1
NCT02320409 Completed Drug: Sulfatinib Healthy Hutchison Medipharma Limited December 2014 Phase 1
NCT02133157 Completed Drug: Sulfatinib Tumor Hutchison Medipharma Limited April 2010 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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