Sulfatinib

SKU: orb1303189

Description

Sulfatinib (KDR-IN-1, HMPL-012) is a highly selective small molecule inhibitor targeting VEGFR1/2/3, FGFR1, and CSF1R with potent activity in the low nanomolar range. It is a valuable research tool for investigating angiogenesis, tumor microenvironment, and related signaling pathways in both cellular and animal models of cancer and inflammatory diseases.

Research Area

Cardiovascular Research, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 1308672-74-3
• MW: 480.58
• Purity: >99.99% (May vary between batches)
• Formula: C₂₄H₂₈N₆O₃S
• SMILES: CN(C)CCNS(=O)(=O)Cc1cccc(Nc2nccc(Oc3ccc4[nH]c(C)cc4c3)n2)c1
• Target: FGFR,VEGFR,Potassium Channel
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.16 mM);DMSO:55 mg/mL (114.45 mM)

Bioactivity

• In Vivo:
  In animal studies, a single oral dose of Sulfatinib effectively inhibits VEGFR2 phosphorylation stimulated by VEGF in lung tissues of nude mice in an exposure-dependent manner. Additionally, a rise in FGF23 plasma levels 24 hours after dosing indicates a suppression of FGFR signaling. Sulfatinib exhibits strong antitumor efficacy across various human xenograft models and significantly reduces CD31 expression, which evidences its potent antiangiogenic effects via the inhibition of VEGFR and FGFR signaling pathways. In the CT-26 syngeneic murine colon cancer model, Sulfatinib achieves moderate tumor growth inhibition following monotherapy. Moreover, after a 10 mg/kg oral dose, the AUC and C_max in mice are 397 ng/mL and 138 ng/mL, respectively .
• In Vitro:
  Sulfatinib inhibits VEGFR1, 2, and 3, FGFR1 and CSF1R kinases with IC 50 s in a range of 1 to 24 nM. Sulfatinib strongly blocks VEGF induced VEGFR2 phosphorylation in HEK293KDR cells and CSF1 stimulated CSF1R phosphorylation in RAW264.7 cells with IC 50 of 2 and 79 nM, respectively. Sulfatinib also attenuates VEGF or FGF stimulated HUVEC cells proliferation with IC 50 < 50 nM . Also, it is a hERG inhibitor with IC 50 of 6.8 μM in CHO cell .

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

KDR-IN-1, KDR, FGFR1, hERG, Sulfatinib

Compound Identifiers

PubChem CID

52920501