2. Neuronal Signaling Protein Tyrosine Kinase/RTK
  3. Trk Receptor
  4. Utatrectinib

Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation and associated tumorigenic behaviors.

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

Utatrectinib

Utatrectinib Chemical Structure

CAS No. : 1079274-94-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Other Forms of Utatrectinib:

Utatrectinib Related Antibodies

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TrkA TrkB TrkC Trk

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation and associated tumorigenic behaviors[1].

In Vitro

Utatrectinib (100 nM, 22 h) inhibits the migration of TrkC-expressing U2SO cells[2].
Utatrectinib (1-10 nM, 24 h) inhibits cell growth in KM12, H460 and H810 cells[3].
Utatrectinib (5 nM, 24 h) inhibits phosphorylation of TRKA/B and downstream signaling in KM12, H460 cells[3].

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

Utatrectinib Related Antibodies

Cell Migration Assay [2]

Cell Line: TrkC-expressing U2SO cells
Concentration: 100 nM
Incubation Time: 22 h
Result: Inhibited cell migration (~2.3-fold, P<0.01).

Western Blot Analysis[3]

Cell Line: KM12, H460 cells
Concentration: 0, 1, 5 nM
Incubation Time: 24 h
Result: Inhibited pTRKA Tyr490 and pAk in KM12 cells.
Inhibited pTRKB Tyr706/707 and pERK in H460 cells.
In Vivo

Utatrectinib (50 mg/kg, p.o., daily) suppresses adenoid cystic carcinoma (ACC) tumor growth in ACCX6 xenograft nu/nu mice model[2].

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

Animal Model: Xenograft nu/nu mice models of human ACC: ACCX6 and ACCX9[2]
Dosage: 50 mg/kg
Administration: Oral administration, daily.
Result: Tumor growth inhibition (TGI): 64% (in ACCX6 model)
Clinical Trial
Molecular Weight

382.39

Formula

C18H19FN8O
CAS No.
Appearance

Solid

Color

Blue to blue-green

SMILES

CC(C)OC1=CC(N2C=NC3=CC=C(N[C@H](C4=NC=C(F)C=N4)C)N=C32)=NN1
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 : 50 mg/mL (130.76 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 2.6151 mL 13.0757 mL 26.1513 mL
5 mM 0.5230 mL 2.6151 mL 5.2303 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
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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: ≥ 1.25 mg/mL (3.27 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (3.27 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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 2.6151 mL 13.0757 mL 26.1513 mL 65.3783 mL
5 mM 0.5230 mL 2.6151 mL 5.2303 mL 13.0757 mL
10 mM 0.2615 mL 1.3076 mL 2.6151 mL 6.5378 mL
15 mM 0.1743 mL 0.8717 mL 1.7434 mL 4.3586 mL
20 mM 0.1308 mL 0.6538 mL 1.3076 mL 3.2689 mL
25 mM 0.1046 mL 0.5230 mL 1.0461 mL 2.6151 mL
30 mM 0.0872 mL 0.4359 mL 0.8717 mL 2.1793 mL
40 mM 0.0654 mL 0.3269 mL 0.6538 mL 1.6345 mL
50 mM 0.0523 mL 0.2615 mL 0.5230 mL 1.3076 mL
60 mM 0.0436 mL 0.2179 mL 0.4359 mL 1.0896 mL
80 mM 0.0327 mL 0.1634 mL 0.3269 mL 0.8172 mL
100 mM 0.0262 mL 0.1308 mL 0.2615 mL 0.6538 mL
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Utatrectinib 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:

Utatrectinib1079274-94-4AZD-7451AZD7451AZD 7451Trk ReceptorTropomyosin related kinase receptorU2SO cellTrkCACCadenoid cystic carcinomatumorKM12H460Inhibitorinhibitorinhibit

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