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Zeteletinib
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Catalog No. T39688Cas No. 2216753-97-6
Alias Zeteletinib, DS-5010, BOS-172738
Zeteletinib (BOS-172738; DS-5010) is a highly potent and selective orally active inhibitor of the RET kinase, demonstrating nanomolar potency against RET and over 300-fold selectivity against VEGFR2. It exhibits remarkable efficacy against wild-type RET, RET V804M/L gatekeeper mutants, and the frequently occurring oncogenic RET mutation M918T, with potent antitumor activity.
Zeteletinib
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Catalog No. T39688Alias Zeteletinib, DS-5010, BOS-172738Cas No. 2216753-97-6
Zeteletinib (BOS-172738; DS-5010) is a highly potent and selective orally active inhibitor of the RET kinase, demonstrating nanomolar potency against RET and over 300-fold selectivity against VEGFR2. It exhibits remarkable efficacy against wild-type RET, RET V804M/L gatekeeper mutants, and the frequently occurring oncogenic RET mutation M918T, with potent antitumor activity.
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Chemical Properties
Storage & Solubility Information
| Description | Zeteletinib (BOS-172738; DS-5010) is a highly potent and selective orally active inhibitor of the RET kinase, demonstrating nanomolar potency against RET and over 300-fold selectivity against VEGFR2. It exhibits remarkable efficacy against wild-type RET, RET V804M/L gatekeeper mutants, and the frequently occurring oncogenic RET mutation M918T, with potent antitumor activity. |
| In vitro | In biochemical assays involving 106 kinases, Zeteletinib (BOS-172738; DS-5010) achieved more than 80% inhibition of RET and platelet-derived growth factor receptor (PDGFR) alpha/beta at a concentration of 193 nM. Zeteletinib displayed potent activity against RET and RET-GKm (V804L) with IC50 values in the single-digit nanomolar range, even in the presence of high ATP concentrations. Conversely, its inhibitory effect on KDR exceeded 1000 nM[1]. |
| In vivo | In a Ba/F3-RET subcutaneous tumor model, Zeteletinib (BOS-172738; DS-5010) administered at 10 mg/kg twice daily (bid) effectively induces tumor regression[1]. Similarly, in an LC2/ad NSCLC xenograft model harboring the RET-CCDC6 fusion gene, Zeteletinib at 1 mg/kg three times daily (tid) induces tumor regression[1]. |
| Synonyms | Zeteletinib, DS-5010, BOS-172738 |
| Molecular Weight | 500.478 |
| Formula | C25H23F3N4O4 |
| Cas No. | 2216753-97-6 |
| Smiles | COc1cc2cc(cnc2cc1OC)-c1ccc(CC(=O)Nc2cc(no2)C(C)(C)C(F)(F)F)cn1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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