Sulfatinib
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MedKoo CAT#: 206205

CAS#: 1308672-74-3

Description: Sulfatinib, also known as surufatinib, 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), with potential antineoplastic and anti-angiogenic activities. Upon oral administration, 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 Structure

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Sulfatinib
CAS# 1308672-74-3
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 206205
Name: Sulfatinib
CAS#: 1308672-74-3
Chemical Formula: C24H28N6O3S
Exact Mass: 480.19
Molecular Weight: 480.587
Elemental Analysis: C, 59.98; H, 5.87; N, 17.49; O, 9.99; S, 6.67

Price and Availability

Size Price Availability Quantity
10mg USD 150 Ready to Ship
25mg USD 250 Ready to ship
50mg USD 400 Ready to ship
100mg USD 650 Ready to ship
200mg USD 1050 Ready to ship
500mg USD 2250 Ready to ship
1g USD 3250 2 Weeks
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Related CAS #: 1308672-74-3   1816307-67-1.  

Synonym: HMPL012; HMPL012; HMPL 012; Sulfatinib; surufatinib;

IUPAC/Chemical Name: N-(2-(dimethylamino)ethyl)-1-(3-((4-((2-methyl-1H-indol-5-yl)oxy)pyrimidin-2-yl)amino)phenyl)methanesulfonamide

InChi Key: TTZSNFLLYPYKIL-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H28N6O3S/c1-17-13-19-15-21(7-8-22(19)27-17)33-23-9-10-25-24(29-23)28-20-6-4-5-18(14-20)16-34(31,32)26-11-12-30(2)3/h4-10,13-15,26-27H,11-12,16H2,1-3H3,(H,25,28,29)

SMILES Code: CC1=CC2=C(N1)C=CC(OC3=NC(NC4=CC(CS(NCCN(C)C)(=O)=O)=CC=C4)=NC=C3)=C2

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:         

Biological target: Sulfatinib is a tyrosine kinase inhibitor against VEGFR1, VEGFR2, VEGFR3, FGFR1 and CSF1R with IC50s of 2 nM, 24 nM, 1 nM, 15 nM and 4 nM, respectively.
In vitro activity: Sulfatinib can inhibit the proliferation, migration, and invasion of osteosarcoma by simultaneously and systematically reverse immunosuppression to immune activation status. Sulfatinib suppressed OS cell migration and invasion by inhibiting EMT by blocking the secretion of bFGF in an autocrine manner. Sulfatinib can suppress OS by modulation of the TME by inhibiting M2 polarization of macrophages. Reference: Front Oncol. 2023 Jun 8;13:1158857. https://pubmed.ncbi.nlm.nih.gov/37361567/
In vivo activity: Sulfatinib was characterized by a high disease control rate and a low disease progression rate, indicating that it could exert a good therapeutic effect on solid tumors. Additionally, sulfatinib showed a lower relative risk for adverse effects. The disease control rate of sulfatinib in solid tumors was 86% and the objective response rate was 16%, while the progressive disease rate was only 9%. Among the adverse events, the incidence of increased levels of (AST) and (ALT) were 24% and 33%, respectively. Reference: Oncol Lett. 2023 May 10;25(6):273. https://pubmed.ncbi.nlm.nih.gov/37216159/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 98.0 203.92

Preparing Stock Solutions

The following data is based on the product molecular weight 480.59 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Liao S, Li J, Gao S, Han Y, Han X, Wu Y, Bi J, Xu M, Bi W. Sulfatinib, a novel multi-targeted tyrosine kinase inhibitor of FGFR1, CSF1R, and VEGFR1-3, suppresses osteosarcoma proliferation and invasion via dual role in tumor cells and tumor microenvironment. Front Oncol. 2023 Jun 8;13:1158857. doi: 10.3389/fonc.2023.1158857. PMID: 37361567; PMCID: PMC10286821. 2. Carra S, Gaudenzi G, Dicitore A, Cantone MC, Plebani A, Saronni D, Zappavigna S, Caraglia M, Candeo A, Bassi A, Persani L, Vitale G. Modeling Lung Carcinoids with Zebrafish Tumor Xenograft. Int J Mol Sci. 2022 Jul 23;23(15):8126. doi: 10.3390/ijms23158126. PMID: 35897702; PMCID: PMC9330857. 3. Cai T, Cheng Y, Du Y, Tan P, Li T, Chen Y, Gao L, Fu W. Efficacy and safety of surufatinib in the treatment of advanced solid tumors: a systematic evaluation and meta‑analysis. Oncol Lett. 2023 May 10;25(6):273. doi: 10.3892/ol.2023.13859. PMID: 37216159; PMCID: PMC10193379. 4. Xu JM, Wang Y, Chen YL, Jia R, Li J, Gong JF, Li J, Qi C, Hua Y, Tan CR, Wang J, Li K, Sai Y, Zhou F, Ren YX, Qing WG, Jia H, Su WG, Shen L. Sulfatinib, a novel kinase inhibitor, in patients with advanced solid tumors: results from a phase I study. Oncotarget. 2017 Jun 27;8(26):42076-42086. doi: 10.18632/oncotarget.14942. PMID: 28159938; PMCID: PMC5522050.
In vitro protocol: 1. Liao S, Li J, Gao S, Han Y, Han X, Wu Y, Bi J, Xu M, Bi W. Sulfatinib, a novel multi-targeted tyrosine kinase inhibitor of FGFR1, CSF1R, and VEGFR1-3, suppresses osteosarcoma proliferation and invasion via dual role in tumor cells and tumor microenvironment. Front Oncol. 2023 Jun 8;13:1158857. doi: 10.3389/fonc.2023.1158857. PMID: 37361567; PMCID: PMC10286821. 2. Carra S, Gaudenzi G, Dicitore A, Cantone MC, Plebani A, Saronni D, Zappavigna S, Caraglia M, Candeo A, Bassi A, Persani L, Vitale G. Modeling Lung Carcinoids with Zebrafish Tumor Xenograft. Int J Mol Sci. 2022 Jul 23;23(15):8126. doi: 10.3390/ijms23158126. PMID: 35897702; PMCID: PMC9330857.
In vivo protocol: 1. Cai T, Cheng Y, Du Y, Tan P, Li T, Chen Y, Gao L, Fu W. Efficacy and safety of surufatinib in the treatment of advanced solid tumors: a systematic evaluation and meta‑analysis. Oncol Lett. 2023 May 10;25(6):273. doi: 10.3892/ol.2023.13859. PMID: 37216159; PMCID: PMC10193379. 2. Xu JM, Wang Y, Chen YL, Jia R, Li J, Gong JF, Li J, Qi C, Hua Y, Tan CR, Wang J, Li K, Sai Y, Zhou F, Ren YX, Qing WG, Jia H, Su WG, Shen L. Sulfatinib, a novel kinase inhibitor, in patients with advanced solid tumors: results from a phase I study. Oncotarget. 2017 Jun 27;8(26):42076-42086. doi: 10.18632/oncotarget.14942. PMID: 28159938; PMCID: PMC5522050.

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