| Size | Price | Stock | Qty |
|---|---|---|---|
| 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 |
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| Additional Infomation |
Zeteletinib is an orally bioavailable selective inhibitor of wild-type, fusion products and mutated forms, including gatekeeper mutations, of the proto-oncogene receptor tyrosine kinase rearranged during transfection (RET), with potential antineoplastic activity. Upon oral administration, zeteletinib selectively binds to and inhibits the activity of RET. This results in an inhibition of cell growth of tumors cells that exhibit increased RET activity. RET overexpression, activating mutations, and fusions result in the upregulation and/or overactivation of RET tyrosine kinase activity in various cancer cell types; dysregulation of RET activity plays a key role in the development and progression of these cancers.
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| Molecular Formula |
C25H23F3N4O4
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|---|---|
| Molecular Weight |
500.469736337662
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| Exact Mass |
500.167
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| CAS # |
2216753-97-6
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| Related CAS # |
Zeteletinib hemiadipate;2375837-06-0
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| PubChem CID |
134391533
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| Appearance |
White to light yellow solid powder
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| LogP |
4.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
36
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| Complexity |
755
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| Defined Atom Stereocenter Count |
0
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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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| InChi Key |
KOLQINCWMXQEOF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H23F3N4O4/c1-24(2,25(26,27)28)21-11-23(36-32-21)31-22(33)7-14-5-6-17(29-12-14)16-8-15-9-19(34-3)20(35-4)10-18(15)30-13-16/h5-6,8-13H,7H2,1-4H3,(H,31,33)
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| Chemical Name |
2-[6-(6,7-dimethoxyquinolin-3-yl)pyridin-3-yl]-N-[3-(1,1,1-trifluoro-2-methylpropan-2-yl)-1,2-oxazol-5-yl]acetamide
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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.
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