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Sulfatinib

Cat. No. M2139
Sulfatinib Structure
Synonym:

HMPL-012; Surufatinib

Size Price Availability Quantity
10mM*1mL in DMSO USD 75  USD75 In stock
5mg USD 90  USD90 In stock
10mg USD 135  USD135 In stock
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Quality Control & Documentation
Biological Activity

Sulfatinib is an orally bioavailable, small molecule inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3, and the fibroblast growth factor receptor type 1 (FGFR1). Sulfatinib binds to and inhibits VEGFRs and FGFR1 thereby inhibiting VEGFR- and FGFR1-mediated signal transduction pathways. This leads to a reduction of angiogenesis and tumor cell proliferation in VEGFR/FGFR1-overexpressing tumor cells. Expression of VEGFRs and FGFR1 may be upregulated in a variety of tumor cell types.

Chemical Information
Molecular Weight 480.58
Formula C24H28N6O3S
CAS Number 1308672-74-3
Solubility (25°C) DMSO 65 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Jianming Xu, et al. Clin Cancer Res. Surufatinib in Advanced Well-Differentiated Neuroendocrine Tumors: A Multicenter, Single-Arm, Open-Label, Phase Ib/II Trial

[2] Jian Ming Xu, et al. Oncotarget. Sulfatinib, a novel kinase inhibitor, in patients with advanced solid tumors: results from a phase I study

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Keywords: Sulfatinib, HMPL-012; Surufatinib supplier, VEGFR/PDGFR, inhibitors, activators


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