2. Protein Tyrosine Kinase/RTK
  3. RET PDGFR
  4. Zeteletinib

Zeteletinib  (Synonyms: BOS-172738; DS-5010)

Cat. No.: HY-139590 Purity: 99.06%
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Zeteletinib (BOS-172738; DS-5010) is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib shows exquisite potency for the wild type RET, RETV804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib has potent antitumor activity.

For research use only. We do not sell to patients.

Zeteletinib Chemical Structure

Zeteletinib Chemical Structure

CAS No. : 2216753-97-6

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5 mg USD 700 In-stock
10 mg USD 1100 In-stock
25 mg USD 2250 In-stock
50 mg USD 3600 In-stock
100 mg USD 5800 In-stock
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Based on 1 publication(s) in Google Scholar

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Zeteletinib Related Antibodies

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Description

Zeteletinib (BOS-172738; DS-5010) is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib shows exquisite potency for the wild type RET, RETV804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib has potent antitumor activity[1][2][3].

IC50 & Target[1]

PDGFR2

 

In Vitro

In biochemical assays of 106 kinases, RET and platelet-derived growth factor receptor (PDGFR) alpha/beta were inhibited more than 80% by 193 nM Zeteletinib (BOS-172738; DS-5010). The IC50 values of Zeteletinib against RET, RET-GKm (V804L) were single digit nano-molar even under a condition of high concentration of ATP; besides it against KDR was more than 1000 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Zeteletinib Related Antibodies
In Vivo

In a Ba/F3-RET subcutaneous tumor model, Zeteletinib (BOS-172738; DS-5010) dosing at 10 mg/kg twice daily (bid) induces tumor regression[1].
In an LC2/ad NSCLC xenograft model, which has the RET-CCDC6 fusion gene, Zeteletinib dosing at 1 mg/kg thrice daily (tid) induced tumor regression[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

500.47

Formula

C25H23F3N4O4
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(CC1=CC=C(C2=CN=C3C=C(C(OC)=CC3=C2)OC)N=C1)NC4=CC(C(C)(C(F)(F)F)C)=NO4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (199.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9981 mL 9.9906 mL 19.9812 mL 49.9530 mL
5 mM 0.3996 mL 1.9981 mL 3.9962 mL 9.9906 mL
10 mM 0.1998 mL 0.9991 mL 1.9981 mL 4.9953 mL
15 mM 0.1332 mL 0.6660 mL 1.3321 mL 3.3302 mL
20 mM 0.0999 mL 0.4995 mL 0.9991 mL 2.4977 mL
25 mM 0.0799 mL 0.3996 mL 0.7992 mL 1.9981 mL
30 mM 0.0666 mL 0.3330 mL 0.6660 mL 1.6651 mL
40 mM 0.0500 mL 0.2498 mL 0.4995 mL 1.2488 mL
50 mM 0.0400 mL 0.1998 mL 0.3996 mL 0.9991 mL
60 mM 0.0333 mL 0.1665 mL 0.3330 mL 0.8326 mL
80 mM 0.0250 mL 0.1249 mL 0.2498 mL 0.6244 mL
100 mM 0.0200 mL 0.0999 mL 0.1998 mL 0.4995 mL
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Zeteletinib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Zeteletinib2216753-97-6BOS-172738 DS-5010BOS172738BOS 172738DS5010DS 5010DS-5010RETPDGFRPlatelet-derived growth factor receptororallyRETV804M/LM918TInhibitorinhibitorinhibit

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