1. Protein Tyrosine Kinase/RTK
  2. FGFR
    VEGFR

Sulfatinib (Synonyms: HMPL-012)

Cat. No.: HY-12297 Purity: 98.34%
Handling Instructions

Sulfatinib (HMPL-012) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC50s of in a range of 1 to 24 nM.

For research use only. We do not sell to patients.

Sulfatinib Chemical Structure

Sulfatinib Chemical Structure

CAS No. : 1308672-74-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 127 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
1 mg USD 80 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 190 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
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Estimated Time of Arrival: December 31
100 mg USD 750 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Sulfatinib (HMPL-012) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC50s of in a range of 1 to 24 nM.

IC50 & Target[1]

VEGFR1

 

VEGFR2

 

VEGFR3

 

FGFR1

 

CSF1R

 

In Vitro

Sulfatinib inhibits VEGFR1, 2, and 3, FGFR1 and CSF1R kinases with IC50s in a range of 1 to 24 nM, and it strongly blocks VEGF induced VEGFR2 phosphorylation in HEK293KDR cells and CSF1 stimulated CSF1R phosphorylation in RAW264.7 cells with IC50 of 2 and 79 nM, respectively. Sulfatinib also attenuates VEGF or FGF stimulated HUVEC cells proliferation with IC50< 50 nM[1]. Also, it is a hERG inhibitor with IC50 of 6.8 μM in CHO cell[2].

In Vivo

In animal studies, a single oral dosing of Sulfatinib inhibits VEGF stimulated VEGFR2 phosphorylation in lung tissues of nude mice in an exposure-dependent manner. Furthermore, elevation of FGF23 levels in plasma 24 hours post dosing suggests suppression of FGFR signaling. Sulfatinib demonstrates potent tumor growth inhibition in multiple human xenograft models and decreases CD31 expression remarkably, suggesting strong inhibition on angiogenesis through VEGFR and FGFR signaling. In a syngeneic murine colon cancer model CT-26, Sulfatinib demonstrates moderate tumor growth inhibition after single agent treatment[1]. After oral dosing of 10 mg/kg, the AUC and Cmax are 397 ng/mL and 138ng/mL in the mouse, respectively[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (62.42 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0808 mL 10.4041 mL 20.8082 mL
5 mM 0.4162 mL 2.0808 mL 4.1616 mL
10 mM 0.2081 mL 1.0404 mL 2.0808 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[2]

The KDR kinase inhibition activity is tested using the the Z-lyte assay kit. The testing system contains 300 ng/mL of recombinant human KDR catalytic domain, 10 μM of ATP, 1 μM of substrate peptide, and a test compound (Sulfatinib) at a series of different concentrations in 384-well plate; total volume is 10 μL. The enzyme inhibition proceeds at room temperature (25°C), for 1 hour at room temperature on the shaker. 5 μL of stop solution is added to stop the reaction[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

The phamacokinetics of Sulfatinib are studied with male ICR mice (n=6 for each group, weight 20-30g) after a single intraveneous and oral dosing at 2.5 and 10mg/kg, respectively. For i.v. dosing formulation, Sulfatinib is dissolved in DMSO (0.25%)-solutol(10%)-ethanol(10%)-physiological saline(79.75%) at the concentration of 0.25 mg/mL. And the p.o. Dosing formulation (1mg/mL) is prepared with 0.5% CMC-Na. After i.v. Or p.o. Dosing, blood samples are collected via the ophthalmic vein at 0 (pre-close), 5, 15, 30 min and 1, 1.5, 2, 4, 8, 24 h, anti-coagulated with heparin-Na. After centrifugation, plasma samples are seprated and protein precipitated with acetonitrilel containing internal standard[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

480.58

Formula

C₂₄H₂₈N₆O₃S

CAS No.

1308672-74-3

SMILES

O=S(CC1=CC=CC(NC2=NC=CC(OC3=CC4=C(NC(C)=C4)C=C3)=N2)=C1)(NCCN(C)C)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Sulfatinib
Cat. No.:
HY-12297
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Sulfatinib

Cat. No.: HY-12297