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Purity: ≥98%
Sulfatinib, formerly 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. Sulfatinib binds to and inhibits FGFR1 and VEGFRs upon oral bioavailable administration, thereby inhibiting signal transduction pathways mediated by FGFR and VEGFR. Tumor cells overexpressing VEGFR/FGFR1 experience a decrease in angiogenesis and tumor cell proliferation as a result. Many types of tumor cells may have elevated expression of FGFR1 and VEGFRs.
| Targets |
VEGFR3 (IC50 = 1 nM); VEGFR1 (IC50 = 2 nM); CSF1R (IC50 = 4 nM); FGFR1 (IC50 = 15 nM); VEGFR2 (IC50 = 24 nM)
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| ln Vitro |
SuLfatinib effectively suppresses VEGF-induced VEGFR2 phosphorylation in HEK293KDR cells and CSF1-stimulated CSF1R phosphorylation in RAW264.7 cells, with IC50s of 2 and 24, respectively. It also inhibits mutations in FGFR1, CSF1R, and VEGFR1, 2, and 3. 79 nanometers. Moreover, SuLfatinib has an IC50<50 nM to suppress HUVEC cell growth that is induced by VEGF or FGF[1]. Furthermore, in CHO cells, it has an IC50 of 6.8 μM, making it a hERG brother [2].
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| ln Vivo |
In animal experiments, VEGF-stimulated VEGFR2 phosphorylation in nude mouse lung tissue was regulated by single-pass SuLfatinib. Furthermore, the suppression of FGFR receptor signaling is indicated by the rise in FGF23 levels in 24 channels after 24 hours. shown robust suppression of angiogenesis via VEGFR and FGFR signaling, as seen by the severe growth inhibition shown in several human xenograft models and the significant reduction of CD31 tumor expression. Sulfatinib demonstrated a moderate reduction in tumor development following a single medication treatment in the syngeneic tumor tumor model CT-26 [1]. The AUC and Cmax in mice were 397 ng/mL and 138 ng/mL, respectively, with a sidewall thickness of 10 mg/kg [1].
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| Enzyme Assay |
The Z-lyte assay kit is utilized to assess the inhibition activity of KDR kinase. Sulfatinib, the test compound, is present in a 384-well plate with varying concentrations, along with 300 ng/mL of recombinant human KDR catalytic domain, 10 μM of ATP, and 1 μM of substrate peptide in the testing system. The total volume is 10 μL. After one hour at room temperature (25°C) on the shaker, the enzyme inhibition process continues. To halt the reaction, 5 μL of stop solution is added[2].
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| Animal Protocol |
Male ICR mice (n = 6 per group; weight 20–30 g) are used to study the phamacokinetics of sulfatinib following a single intravenous and oral dose of 2.5 and 10 mg/kg, respectively. Sulfatinib is dissolved in DMSO (0.25%)-solutol (10%)-ethanol (10%)-physiological saline (797.75%) at a concentration of 0.25 mg/mL for intravenous dosing formulation. Additionally, 0.5% CMC-Na is used to prepare the p.o. Dosing formulation (1 mg/mL). Following intravenous or PO dosage, blood is drawn via the ophthalmic vein at 0 (pre-close), 5, 15, 30 minutes, and 1, 1.5, 2, 4, 8, and 24 hours. The blood is then anticoagulated using heparin-Na. Following centrifugation, plasma samples are separated, and protein is precipitated using an internal standard containing acetonitrilel[2].
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| References | |
| Additional Infomation |
Surufatinib is under investigation in clinical trial NCT02588170 (Phase III Study of Surufatinib in Treating Advanced Extrapancreatic Neuroendocrine Tumors).
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), 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. Drug Indication Treatment of all conditions included in the category of malignant neoplasms (except central nervous system tumours, haematopoietic and lymphoid tissue neoplasms), Treatment of malignant neoplasms of haematopoietic and lymphoid tissue |
| Molecular Formula |
C24H28N6O3S
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|---|---|
| Molecular Weight |
480.587
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| Exact Mass |
480.194
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| Elemental Analysis |
C, 59.98; H, 5.87; N, 17.49; O, 9.99; S, 6.67
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| CAS # |
1308672-74-3
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| Related CAS # |
1308672-74-3;1816307-67-1
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| PubChem CID |
52920501
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
712.9±70.0 °C at 760 mmHg
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| Flash Point |
385.0±35.7 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.658
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| LogP |
3.06
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
34
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| Complexity |
733
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C([H])([H])C1C([H])=C([H])C([H])=C(C=1[H])N([H])C1=NC([H])=C([H])C(=N1)OC1C([H])=C([H])C2=C(C=1[H])C([H])=C(C([H])([H])[H])N2[H])(N([H])C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])[H])(=O)=O
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| InChi Key |
TTZSNFLLYPYKIL-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
N-[2-(dimethylamino)ethyl]-1-[3-[[4-[(2-methyl-1H-indol-5-yl)oxy]pyrimidin-2-yl]amino]phenyl]methanesulfonamide
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| Synonyms |
HMPL012; HMPL012; HMPL 012; surufatinib; Sulfatinib
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~96 mg/mL (~199.8 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.33 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.33 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.33 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0808 mL | 10.4039 mL | 20.8078 mL | |
| 5 mM | 0.4162 mL | 2.0808 mL | 4.1616 mL | |
| 10 mM | 0.2081 mL | 1.0404 mL | 2.0808 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05077384 | Recruiting | Drug: Surufatinib | Neuroendocrine Tumors Non-hematologic Malignancy |
Hutchison Medipharma Limited | September 2, 2021 | Phase 1 Phase 2 |
| NCT04579679 | Active Recruiting |
Drug: Surufatinib | Neuroendocrine Tumours Small Intestinal NET |
Hutchmed | August 13, 2021 | Phase 2 |
| NCT05171439 | Recruiting | Drug: Surufatinib | Hepatocellular Carcinoma | he Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School |
March 1, 2022 | Phase 2 |
| NCT05590572 | Not yet recruiting | Drug: Sulfatinib Drug: Etoposide |
Osteosarcoma | Second Affiliated Hospital, School of Medicine, Zhejiang University |
January 2023 | Phase 1 Phase 2 |
| NCT02549937 | Active Recruiting |
Drug: surufatinib | Tumors | Hutchison Medipharma Limited | November 2015 | Phase 1 Phase 2 |
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