Size | Price | Stock | Qty |
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1mg |
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5mg |
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Other Sizes |
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Targets |
PDGFR2
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ln Vitro |
193 nM Zeteletinib (BOS-172738; DS-5010) inhibited RET and platelet-derived growth factor receptor (PDGFR) alpha/beta by more than 80% in biochemical assays of 106 kinases. Even in the presence of high ATP concentrations, Zeteletinib's IC50 values against RET and RET -GKm (V804L) were single digit nano-molar; in addition, it was more than 1000 nM against KDR[1].
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ln Vivo |
Zeteletinib (BOS-172738; DS-5010) dosed at 10 mg/kg twice daily (bid) causes tumor shrinkage in a Ba/F3-RET subcutaneous tumor model[1]. Tumor regression was observed in an LC2/ad NSCLC xenograft model with the RET-CCDC6 fusion gene when zeteletinib was dosed at 1 mg/kg three times a day (tid)[1].
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References |
[1]. Yasuyuki Kaneta, et al.Abstract B173: Preclinical characterization and antitumor efficacy of DS-5010, a highly potent and selective RET inhibitor. MOLECULAR CANCERTHERAPEUTICS. January 2018, Volume 17, Issue 1.
[2]. Patrick Schoffski, et al. BOS172738, a highly potent and selective RET inhibitor, for the treatment of RET-altered tumors including RET-fusion+ NSCLC and RET-mutant MTC: Phase 1 study results. Journal of Clinical Oncology 39, no. 15_suppl (May 20, 2021) 3 [3]. Kyaw Z Thein, et al. Precision therapy for RET-altered cancers with RET inhibitors. Trends Cancer. 2021 Dec;7(12):1074-1088. |
Molecular Formula |
C25H23F3N4O4
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Molecular Weight |
500.47
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CAS # |
2216753-97-6
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Related CAS # |
Zeteletinib hemiadipate;2375837-06-0
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
FC(C(C)(C)C1C=C(NC(CC2=CN=C(C=C2)C2=CN=C3C=C(C(=CC3=C2)OC)OC)=O)ON=1)(F)F
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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: 100 mg/mL (199.81 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.00 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 25.0 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: ≥ 2.5 mg/mL (5.00 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 25.0 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: ≥ 2.5 mg/mL (5.00 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 | 1.9981 mL | 9.9906 mL | 19.9812 mL | |
5 mM | 0.3996 mL | 1.9981 mL | 3.9962 mL | |
10 mM | 0.1998 mL | 0.9991 mL | 1.9981 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.