Product Details
| Product Name:
Sulfatinib |
CAS No.:
1308672-74-3 |
| Purity:
98.93% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | Sulfatinib |
| Description | Sulfatinib (KDR-IN-1) (HMPL-012) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC 50 s ranging from 1 to 24 nM. |
| 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 [1]. Also, it is a hERG inhibitor with IC 50 of 6.8 μM in CHO cell [2]. |
| 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 [1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 55 mg/mL (114.45 mM)
|
| Keywords | Sulfatinib |
| Inhibitors Related | Sorafenib | Ferulic Acid |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States