2. Protein Tyrosine Kinase/RTK
  3. ROS Kinase
  4. Zidesamtinib

Zidesamtinib  (Synonyms: NVL-520)

Cat. No.: HY-152292 Purity: 99.55%
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Zidesamtinib (NVL-520) is a potent, selective, orally active and brain-penetrant inhibitor of diverse ROS1 fusions and resistance mutations, with IC50s of 0.7 and 7.9 nM for wild-type ROS1 and ROS1 G2032R, respectively, and spares TRK inhibition. Zidesamtinib can be used for the research of cancer.

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

Zidesamtinib Chemical Structure

Zidesamtinib Chemical Structure

CAS No. : 2739829-00-4

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1 mg USD 580 In-stock
5 mg USD 1450 In-stock
10 mg USD 2320 In-stock
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Based on 1 publication(s) in Google Scholar

Zidesamtinib Related Antibodies

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Description

Zidesamtinib (NVL-520) is a potent, selective, orally active and brain-penetrant inhibitor of diverse ROS1 fusions and resistance mutations, with IC50s of 0.7 and 7.9 nM for wild-type ROS1 and ROS1 G2032R, respectively, and spares TRK inhibition. Zidesamtinib can be used for the research of cancer[1].

In Vitro

Zidesamtinib (72 h) inhibits the growth of seven cell lines expressing wild-type ROS1 fusions, with average IC50s of 0.4 nM[1].
Zidesamtinib (72 h) inhibits the growth of six cell lines harboring ROS1 fusions with the G2032R mutation, with average IC50s of 1.6 nM[1].
Zidesamtinib (72 h) potently inhibits the non-G2032R ROS1 mutants, with IC50s ≤ 1.5 nM[1].
Zidesamtinib (10-1000 nM; 4 weeks) suppresses colony formation in NIH3T3 cells expressing wild-type ROS1 fusions and expressing ROS1 fusions with G2032R[1].

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

Zidesamtinib Related Antibodies
In Vivo

Zidesamtinib (0.04-15 mg/kg; p.o. twice daily for 28 d) induces tumor regression at all doses ≥0.2 mg/kg in wild-type ROS1 xenograft models[1].

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

Animal Model: Female athymic Nude-Foxn1nu mice were implanted subcutaneously with tumor fragments from model CTG-0848[1]
Dosage: 0.04, 0.2, 1, 5, 15 mg/kg
Administration: Oral gavage twice daily for 21 days
Result: Inhibited the tumor volumes.
Clinical Trial
Molecular Weight

419.45

Formula

C22H22FN7O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CCN1C2=C(C=N1)CC3=NN(C)N=C3C4=CC=C(F)C=C4[C@H](OC5=C(N)N=CC2=C5)C
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 (119.20 mM; ultrasonic and warming and heat to 65°C; 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 2.3841 mL 11.9204 mL 23.8407 mL
5 mM 0.4768 mL 2.3841 mL 4.7681 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: ≥ 1.25 mg/mL (2.98 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 (2.98 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 2.3841 mL 11.9204 mL 23.8407 mL 59.6019 mL
5 mM 0.4768 mL 2.3841 mL 4.7681 mL 11.9204 mL
10 mM 0.2384 mL 1.1920 mL 2.3841 mL 5.9602 mL
15 mM 0.1589 mL 0.7947 mL 1.5894 mL 3.9735 mL
20 mM 0.1192 mL 0.5960 mL 1.1920 mL 2.9801 mL
25 mM 0.0954 mL 0.4768 mL 0.9536 mL 2.3841 mL
30 mM 0.0795 mL 0.3973 mL 0.7947 mL 1.9867 mL
40 mM 0.0596 mL 0.2980 mL 0.5960 mL 1.4900 mL
50 mM 0.0477 mL 0.2384 mL 0.4768 mL 1.1920 mL
60 mM 0.0397 mL 0.1987 mL 0.3973 mL 0.9934 mL
80 mM 0.0298 mL 0.1490 mL 0.2980 mL 0.7450 mL
100 mM 0.0238 mL 0.1192 mL 0.2384 mL 0.5960 mL
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Zidesamtinib 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:

Zidesamtinib2739829-00-4NVL-520NVL520NVL 520ROS KinaseROS1 fusionsresistance mutationsROS1 G2032RTRKcancerInhibitorinhibitorinhibit

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