Referencia número: HY-12297

Sulfatinib

(Synonyms: Surufatinib; HMPL-012)

2 Cited Publications

Revisión del cliente

Based on 2 publication(s) in Google Scholar

Sulfatinib (Surufatinib) 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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Pureza: 99.52%
No. CAS: 1308672-74-3
Fòrmula: C₂₄H₂₈N₆O₃S
Peso molecular:480.58

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Sulfatinib Chemical Structure

No. CAS: 1308672-74-3

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (2)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

Sulfatinib (Surufatinib) 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

Ver todos los productos específicos de isoformas VEGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
HUVEC	IC₅₀	<50 nM Compound: HMPL-012	Antiproliferative activity against FGF stimulated HUVEC cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against FGF stimulated HUVEC cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 36335744]
HUVEC	IC₅₀	<50 nM Compound: HMPL-012	Antiproliferative activity against VEGF stimulated HUVEC cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against VEGF stimulated HUVEC cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 36335744]

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].

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

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 C_max are 397 ng/mL and 138ng/mL in the mouse, respectively^[1].

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

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 1308672-74-3
Appearance Solid
Peso molecular 480.58
Fòrmula C₂₄H₂₈N₆O₃S
Color White to off-white
SMILES

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

Surufatinib; HMPL-012
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

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Journal Impact Factor

Mol Syst Biol

Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]

2024 Jan;20(1):28-55. PMID: 38177929
Int J Mol Sci

Modeling Lung Carcinoids with Zebrafish Tumor Xenograft. [Abstract]

2022 Jul 23;23(15):8126. PMID: 35897702

Solvente y solubilidad

In Vitro:

DMSO : ≥ 100 mg/mL (208.08 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocolo

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].

MedChemExpress (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].

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (272 KB)
SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. PCT Int. Appl. (2011), WO 2011060746 A1 20110526.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0808 mL	10.4041 mL	20.8082 mL	52.0205 mL
	5 mM	0.4162 mL	2.0808 mL	4.1616 mL	10.4041 mL
	10 mM	0.2081 mL	1.0404 mL	2.0808 mL	5.2020 mL
	15 mM	0.1387 mL	0.6936 mL	1.3872 mL	3.4680 mL
	20 mM	0.1040 mL	0.5202 mL	1.0404 mL	2.6010 mL
	25 mM	0.0832 mL	0.4162 mL	0.8323 mL	2.0808 mL
	30 mM	0.0694 mL	0.3468 mL	0.6936 mL	1.7340 mL
	40 mM	0.0520 mL	0.2601 mL	0.5202 mL	1.3005 mL
	50 mM	0.0416 mL	0.2081 mL	0.4162 mL	1.0404 mL
	60 mM	0.0347 mL	0.1734 mL	0.3468 mL	0.8670 mL
	80 mM	0.0260 mL	0.1301 mL	0.2601 mL	0.6503 mL
	100 mM	0.0208 mL	0.1040 mL	0.2081 mL	0.5202 mL

Keywords

Sulfatinib

2 Cited Publications

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Sulfatinib

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

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NMPA-Approved Drug Library

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Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

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Anti-Colorectal Cancer Compound Library

FDA-Approved Anticancer Drug Library

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Anti-Pulmonary Fibrosis Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Cancer Approved Drug Library

Posttranslational Modification Library

FDA Kinase Inhibitor Library

Publications Citing Use of MedChemExpress (MCE) Sulfatinib

Ver todos los productos específicos de isoformas VEGFR

Actividad biológica

Chemical Information

Publications (2)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Sulfatinib Related Classifications

HY-12297 Related Classifications