2. Protein Tyrosine Kinase/RTK Apoptosis
  3. RET Apoptosis
  4. Vepafestinib

Vepafestinib  (Synonyms: TAS0953/HM06)

Cat. No.: HY-132846 Purity: 98.61%
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Vepafestinib (TAS0953/HM06) is a next-generation brain-penetrant, selective and orally active RET inhibitor with an IC50 value of 0.33 nM. Vepafestinib inhibits the phosphorylation of RET and its downstream signaling pathways, thus blocking the growth and signal transduction of tumor cells and inducing cell cycle arrest and apoptosis. Vepafestinib can be used in the research of various RET-driven cancers, such as non-small cell lung cancer, thyroid cancer and other disease areas.

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

Vepafestinib Chemical Structure

Vepafestinib Chemical Structure

CAS No. : 2129515-96-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
Solid
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Based on 1 publication(s) in Google Scholar

Vepafestinib Related Antibodies

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Description

Vepafestinib (TAS0953/HM06) is a next-generation brain-penetrant, selective and orally active RET inhibitor with an IC50 value of 0.33 nM. Vepafestinib inhibits the phosphorylation of RET and its downstream signaling pathways, thus blocking the growth and signal transduction of tumor cells and inducing cell cycle arrest and apoptosis. Vepafestinib can be used in the research of various RET-driven cancers, such as non-small cell lung cancer, thyroid cancer and other disease areas[1].

In Vitro

Vepafestinib (0.01-10000 nM; 96 h) inhibits growth of all tumor cell lines[1].
Vepafestinib (5-500 nM; 2 h) inhibits cell growth and blocks the phosphorylation of RET and ERK in Ba/F3 cells expressing KIF5B-RET or its mutants[1].
Vepafestinib (100 nM; 6-24 h) inhibits the phosphorylation of RET, AKT, S6, ERK1 and ERK2 in LUAD-0002AS1 cells. And ownregulates the cell cycle regulator cyclin D1, induces the expression of apoptosis markers.

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

Vepafestinib Related Antibodies

Cell Viability Assay[1]

Cell Line: LUAD-0002AS1, TT, ECLC5B cells
Concentration: 0.01 nM, 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM, 10000 nM
Incubation Time: 96 h
Result: Inhibited growth of all tumor cell lines.

Western Blot Analysis[1]

Cell Line: Ba/F3 cells expressing KIF5B-RET or mutants
Concentration: 5 nM, 50 nM and 500 nM
Incubation Time: 2 h
Result: Inhibited the growth of Ba/F3 cells expressing KIF5B-RET or mutants.
Blocked the phosphorylation of RET and ERK, with near-complete inhibition of phosphorylation of RETG810R, RETG810S and RETG810C at 100 nM.

Western Blot Analysis[1]

Cell Line: LUAD-0002AS1 cells
Concentration: 100 nM
Incubation Time: 24 h
Result: Downregulated the cell cycle regulator cyclin D1, increased the expression of the cell cycle inhibitor p27, and downregulated p21.
Induced the expression of apoptosis markers such as cleaved PARP (c-PARP), BIM and PUMA.
In Vivo

Vepafestinib (12.5-100 mg/kg; oral administration) significantly inhibits tumor growth and has no significant effect on animal body weight in mouse models implanted with NIH-3T3-RET, ECLC5B, LC-2/ad, LUAD-0057AS1, LUAD-0087AS2, LUAD-0077AS1 cells or tumors[1].
Vepafestinib (10-50 mg/kg; oral administration; twice daily; continuous administration) effectively inhibits tumor growth without affecting animal body weight in mouse models of Ba/F3 KIF5B-RETWT or Ba/F3 KIF5B-RETG810R allograft tumors[1].

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

Animal Model: Female athymic nude mice (6-8 weeks old), implanted subcutaneously with NIH-3T3 cells expressing CCDC6-RET fusion complementary DNA[1].
Dosage: 12.5 mg/kg, 25 mg/kg, 50 mg/kg, 100 mg/kg
Administration: Oral gavage, once or twice daily, for 7 days
Result: Resulted in a dose-dependent decrease in the growth of NIH-3T3-RET xenograft tumors. All dosages tested significantly reduced tumor volume, and there was no statistically significant reduction in animal weight.
Animal Model: Female NOD-SCID gamma (NSG) mice (6-8 weeks old), implanted subcutaneously with ECLC5B xenograft tumors[1]
Dosage: 25 mg/kg, 50 mg/kg, 100 mg/kg
Administration: Oral gavage, once or twice daily, for 35 days
Result: Significantly reduced ECLC5B xenograft tumor growth, and there was no significant reduction in animal weight.
Animal Model: Female NSG mice (6-8 weeks old), implanted subcutaneously with LUAD-0057AS1 patient-derived xenograft (PDX) tumors[1]
Dosage: 50 mg/kg, 100 mg/kg
Administration: Oral gavage, once or twice daily, for 21 days
Result: Significantly reduced the volume of LUAD-0057AS1 PDX tumors, and there was no significant reduction in animal weight.
Clinical Trial
Molecular Weight

474.55

Formula

C26H30N6O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C(C#CCN2CCOCC2)N(C3(C)CC3)C4=NC=NC(N)=C41)NC5=CC=C(COC)C=C5
Shipping

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

DMSO : 50 mg/mL (105.36 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 2.1073 mL 10.5363 mL 21.0726 mL
5 mM 0.4215 mL 2.1073 mL 4.2145 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
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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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: ≥ 1 mg/mL (2.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
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 2.1073 mL 10.5363 mL 21.0726 mL 52.6815 mL
5 mM 0.4215 mL 2.1073 mL 4.2145 mL 10.5363 mL
10 mM 0.2107 mL 1.0536 mL 2.1073 mL 5.2681 mL
15 mM 0.1405 mL 0.7024 mL 1.4048 mL 3.5121 mL
20 mM 0.1054 mL 0.5268 mL 1.0536 mL 2.6341 mL
25 mM 0.0843 mL 0.4215 mL 0.8429 mL 2.1073 mL
30 mM 0.0702 mL 0.3512 mL 0.7024 mL 1.7560 mL
40 mM 0.0527 mL 0.2634 mL 0.5268 mL 1.3170 mL
50 mM 0.0421 mL 0.2107 mL 0.4215 mL 1.0536 mL
60 mM 0.0351 mL 0.1756 mL 0.3512 mL 0.8780 mL
80 mM 0.0263 mL 0.1317 mL 0.2634 mL 0.6585 mL
100 mM 0.0211 mL 0.1054 mL 0.2107 mL 0.5268 mL
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Vepafestinib 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:

Vepafestinib2129515-96-2TAS0953/HM06RETApoptosisbrain-penetrantorally activeRET-driven cancerscell cycle arrestInhibitorinhibitorinhibit

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