1. Protein Tyrosine Kinase/RTK
  2. FGFR
    VEGFR
  3. Sulfatinib

Sulfatinib (Synonyms: HMPL-012)

製品番号: HY-12297 純度: 98.01%
取扱説明書

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.

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Sulfatinib 構造式

Sulfatinib 構造式

CAS 番号 : 1308672-74-3

容量 価格(税別) 在庫状況 数量
10 mM * 1 mL in DMSO USD 95 在庫あり
Estimated Time of Arrival: December 31
1 mg USD 50 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 90 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 120 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 290 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 450 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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製品説明

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

 

体外実験

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].

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

体内実験

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].

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

臨床実験
分子量

480.58

分子式

C₂₄H₂₈N₆O₃S

CAS 番号

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 100 mg/mL (208.08 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.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.33 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.33 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.33 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献
キナーゼ実験
[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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

動物実験
[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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献
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Keywords:

SulfatinibHMPL-012HMPL012HMPL 012FGFRVEGFRFibroblast growth factor receptorVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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製品名:
Sulfatinib
製品番号:
HY-12297
数量:
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