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Sulfatinib

CAS# 1308672-74-3

Sulfatinib

Catalog No. BCC8811----Order now to get a substantial discount!

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Quality Control of Sulfatinib

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Chemical structure

Sulfatinib

3D structure

Chemical Properties of Sulfatinib

Cas No. 1308672-74-3 SDF Download SDF
PubChem ID 52920501 Appearance Powder
Formula C24H25ClFN5O3 M.Wt 485.9
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Surufatinib
Solubility DMSO : ≥ 100 mg/mL (208.08 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name N-[2-(dimethylamino)ethyl]-1-[3-[[4-[(2-methyl-1H-indol-5-yl)oxy]pyrimidin-2-yl]amino]phenyl]methanesulfonamide
SMILES CC1=CC2=C(N1)C=CC(=C2)OC3=NC(=NC=C3)NC4=CC=CC(=C4)CS(=O)(=O)NCCN(C)C
Standard InChIKey TTZSNFLLYPYKIL-UHFFFAOYSA-N
Standard InChI 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)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Sulfatinib Dilution Calculator

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Sulfatinib Molarity Calculator

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Preparing Stock Solutions of Sulfatinib

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.058 mL 10.2902 mL 20.5804 mL 41.1607 mL 51.4509 mL
5 mM 0.4116 mL 2.058 mL 4.1161 mL 8.2321 mL 10.2902 mL
10 mM 0.2058 mL 1.029 mL 2.058 mL 4.1161 mL 5.1451 mL
50 mM 0.0412 mL 0.2058 mL 0.4116 mL 0.8232 mL 1.029 mL
100 mM 0.0206 mL 0.1029 mL 0.2058 mL 0.4116 mL 0.5145 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on Sulfatinib

Sulfatinib, a novel kinase inhibitor, in patients with advanced solid tumors: results from a phase I study.[Pubmed:28159938]

Oncotarget. 2017 Jun 27;8(26):42076-42086.

Sulfatinib is a small molecule kinase inhibitor that targets tumor angiogenesis and immune modulation. This phase I study (NCT02133157) investigated the safety, pharmacokinetic characteristics, and preliminary anti-tumor activity of Sulfatinib in patients with advanced solid tumors. The study included a dose-escalation phase (50-350 mg/day, 28-day cycle) with a Fibonacci (3+3) design, and a tumor-specific expansion phase investigating the tumor response to treatment. Two Sulfatinib formulations were assessed: formulation 1 (5, 25, and 50 mg capsules) and formulation 2 (50 and 200 mg capsules). Seventy-seven Chinese patients received oral Sulfatinib; the maximum tolerated dose was not reached. Dose-limiting toxicities included abnormal hepatic function and coagulation tests, and upper gastrointestinal hemorrhage. The most common treatment-related adverse events were proteinuria, hypertension and diarrhea. Among 34 patients receiving Sulfatinib formulation 2, one patient with hepatocellular carcinoma and eight with neuroendocrine tumors exhibited a partial response; 15 had stable disease. The objective response rate was 26.5% (9/34) and the disease control rate was 70.6% (24/34). Pharmacokinetic, safety, and efficacy data supported continuous oral administration of Sulfatinib at 300 mg as the recommended phase II dose. Sulfatinib exhibited an acceptable safety profile and encouraging antitumor activity in patients with advanced solid tumors, particularly neuroendocrine tumors.

Description

Sulfatinib (HMPL-012) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC50s of in a range of 1 to 24 nM.

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