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MedKoo Cat#: 206205 | Name: Sulfatinib
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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

Sulfatinib
Sulfatinib
CAS#1308672-74-3

Theoretical Analysis

MedKoo Cat#: 206205

Name: Sulfatinib

CAS#: 1308672-74-3

Chemical Formula: C24H28N6O3S

Exact Mass: 480.1944

Molecular Weight: 480.59

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 150.00 Ready to Ship
25mg USD 250.00 Ready to ship
50mg USD 400.00 Ready to ship
100mg USD 650.00 Ready to ship
200mg USD 1,050.00 Ready to ship
500mg USD 2,250.00 Ready to ship
1g USD 3,250.00 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/
Solvent mg/mL mM
Solubility
DMSO 98.0 203.92
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.
 1: Lin Q, Dai S, Qu L, Lin H, Guo M, Wei H, Chen Y, Chen X. Structural basis and selectivity of sulfatinib binding to FGFR and CSF-1R. Commun Chem. 2024 Jan 3;7(1):3. doi: 10.1038/s42004-023-01084-0. PMID: 38172256; PMCID: PMC10764862. 2: 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. 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: Saronni D, Gaudenzi G, Dicitore A, Carra S, Cantone MC, Borghi MO, Barbieri A, Mignani L, Hofland LJ, Persani L, Vitale G. Preclinical Evaluation of Novel Tyrosine-Kinase Inhibitors in Medullary Thyroid Cancer. Cancers (Basel). 2022 Sep 13;14(18):4442. doi: 10.3390/cancers14184442. PMID: 36139603; PMCID: PMC9497079. 5: 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. 6: Xu J. Current treatments and future potential of surufatinib in neuroendocrine tumors (NETs). Ther Adv Med Oncol. 2021 Aug 31;13:17588359211042689. doi: 10.1177/17588359211042689. PMID: 34484432; PMCID: PMC8411625. 7: Lu X, Yan S, Koral KA, Chen Z. Surufatinib for the treatment of advanced extrapancreatic neuroendocrine tumors. Expert Rev Anticancer Ther. 2021 Sep;21(9):917-926. doi: 10.1080/14737140.2021.1944110. Epub 2021 Jun 29. PMID: 34142932. 8: Shi D, Dong GQ, Shen KR, Pan Y, Wei SM, Chen Y, Yu RS. Primary cystic and solid neuroendocrine tumor of the retroperitoneum: A case report. Medicine (Baltimore). 2021 Jan 15;100(2):e24054. doi: 10.1097/MD.0000000000024054. PMID: 33466160; PMCID: PMC7808506. 9: Xu J, Shen L, Zhou Z, Li J, Bai C, Chi Y, Li Z, Xu N, Li E, Liu T, Bai Y, Yuan Y, Li X, Wang X, Chen J, Ying J, Yu X, Qin S, Yuan X, Zhang T, Deng Y, Xiu D, Cheng Y, Tao M, Jia R, Wang W, Li J, Fan S, Peng M, Su W. Surufatinib in advanced extrapancreatic neuroendocrine tumours (SANET-ep): a randomised, double-blind, placebo-controlled, phase 3 study. Lancet Oncol. 2020 Nov;21(11):1500-1512. doi: 10.1016/S1470-2045(20)30496-4. Epub 2020 Sep 20. PMID: 32966811. 10: Xu J, Li J, Bai C, Xu N, Zhou Z, Li Z, Zhou C, Jia R, Lu M, Cheng Y, Mao C, Wang W, Cheng K, Su C, Hua Y, Qi C, Li J, Wang W, Li K, Sun Q, Ren Y, Su W. Surufatinib in Advanced Well-Differentiated Neuroendocrine Tumors: A Multicenter, Single-Arm, Open-Label, Phase Ib/II Trial. Clin Cancer Res. 2019 Jun 15;25(12):3486-3494. doi: 10.1158/1078-0432.CCR-18-2994. Epub 2019 Mar 4. PMID: 30833272. 11: Grillo F, Florio T, Ferraù F, Kara E, Fanciulli G, Faggiano A, Colao A; NIKE Group. Emerging multitarget tyrosine kinase inhibitors in the treatment of neuroendocrine neoplasms. Endocr Relat Cancer. 2018 Sep;25(9):R453-R466. doi: 10.1530/ERC-17-0531. Epub 2018 May 16. PMID: 29769293. 12: 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.