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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Purity: ≥98%
Futibatinib (formerly also known as TAS 120; TAS-120) is a novel, potent, irreversible and orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with potential anticancer activity. Its IC50 values for inhibiting FGFR 1-4 are 3.9, 1.3, 1.6, and 8.3 nM, in that order. TAS-120 specifically and irreversibly binds to FGFR, inhibiting it. This may lead to increased cell death in tumor cells overexpressing FGFR, as well as the inhibition of the FGFR-mediated signal transduction pathway and tumor cell proliferation. Many different types of tumor cells express FGFR, a receptor tyrosine kinase that is critical to the growth, differentiation, and survival of tumor cells.
Targets |
FGFR1 (IC50 = 3.9 nM); FGFR2 (IC50 = 1.3 nM); FGFR3 (IC50 = 1.6 nM); FGFR4 (IC50 = 8.3 nM); wild-type FGFR2 (IC50 = 0.3 nM); FGFR2 V5651 (IC50 = 1-3 nM); FGFR2 N550H (IC50 = 3.6 nM); FGFR2 E566G (IC50 = 2.4 nM)
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ln Vitro |
Futibatinib (TAS-120) is a permanent fibroblast growth factor receptor (FGFR) inhibitor that inhibits all four FGFR subtypes, with enzyme half-lives (IC50) for FGFR1, FGFR2, FGFR3, and FGFR4 being 1.8 nM, 1.4 nM, 1.6 nM, and 3.7 nM, respectively.
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ln Vivo |
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Cell Assay |
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Animal Protocol |
The old 6-week-old male nude rats with an intermittent administration schedule are transplanted to the right chest of the anti-tumor effect human gastric cancer strain (OCUM-2MD3). Measuring the tumor's volume after implantation and its major and minor axes in millimeters: The day 0 of the days that are conducted in groups of (n=5) is determined by allocating the mouse average TV to each group after the tumor volume TV has been calculated. Futibatinib (TAS-120) is prepared so that it contains 3 mg/kg/day and 30 mg/kg/day. 3 mg/kg/day is taken orally every day, while 30 mg/kg/day is taken orally every other day. 100 mg/kg/day is taken orally twice a week starting on day 1, with a 14-day evaluation period and a 15-day final valuation date.
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References |
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Molecular Formula |
C22H22N6O3
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Molecular Weight |
418.4485
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Exact Mass |
418.18
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Elemental Analysis |
C, 63.15; H, 5.30; N, 20.08; O, 11.47
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CAS # |
1448169-71-8
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Appearance |
Off-white to light beige solid powder
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SMILES |
COC1=CC(=CC(=C1)C#CC2=NN(C3=NC=NC(=C23)N)[C@H]4CCN(C4)C(=O)C=C)OC
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InChi Key |
KEIPNCCJPRMIAX-HNNXBMFYSA-N
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InChi Code |
InChI=1S/C22H22N6O3/c1-4-19(29)27-8-7-15(12-27)28-22-20(21(23)24-13-25-22)18(26-28)6-5-14-9-16(30-2)11-17(10-14)31-3/h4,9-11,13,15H,1,7-8,12H2,2-3H3,(H2,23,24,25)/t15-/m0/s1
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Chemical Name |
1-[(3S)-3-[4-amino-3-[2-(3,5-dimethoxyphenyl)ethynyl]pyrazolo[3,4-d]pyrimidin-1-yl]pyrrolidin-1-yl]prop-2-en-1-one
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Synonyms |
Futibatinib; TAS-120; TAS 120; TAS120
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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: ≥ 29 mg/mL (~69.3 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.97 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (4.97 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 (4.97 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 | 2.3898 mL | 11.9489 mL | 23.8977 mL | |
5 mM | 0.4780 mL | 2.3898 mL | 4.7795 mL | |
10 mM | 0.2390 mL | 1.1949 mL | 2.3898 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 |
NCT04189445 | Active Recruiting |
Drug: Futibatinib | Advanced or Metastatic Solid Tumor Myeloid or Lymphoid Neoplasms (MLN) |
Taiho Oncology, Inc. | August 24, 2020 | Phase 2 |
NCT04093362 | Active Recruiting |
Drug: TAS-120 Drug: Cisplatin/Gemcitabine |
Advanced Cholangiocarcinoma FGFR2 Gene Rearrangements |
Taiho Oncology, Inc. | March 1, 2020 | Phase 3 |
NCT04024436 | Active Recruiting |
Drug: Futibatinib Drug: Futibatinib plus Fulvestrant |
Metastatic Breast Cancer FGFR 1 High Amplification Metastatic Melanoma |
Taiho Oncology, Inc. | August 30, 2019 | Phase 2 |
NCT02052778 | Active Recruiting |
Drug: Futibatinib | Urothelial Cancer Primary CNS Tumors |
Taiho Oncology, Inc. | July 2014 | Phase 1 Phase 2 |
NCT05615818 | Not yet recruiting | Drug: Futibatinib Drug: Ivosidenib |
Biliary Tract Neoplasms | UNICANCER | January 2024 | Phase 3 |
TAS-120 is clinically effective in FGFR2 fusion-positive ICC patients whose tumors acquired resistance to BGJ398 or Debio1347. Cancer Discov . 2019 Aug;9(8):1064-1079. td> |
Structural modeling of secondary FGFR2 kinase domain mutations with TAS-120. Cancer Discov . 2019 Aug;9(8):1064-1079. td> |