2. Protein Tyrosine Kinase/RTK
  3. Src
  4. CH6953755

CH6953755 is a potent, orally active and selective YES1 kinase (a member of the SRC family) inhibitor with an IC50 of 1.8 nM. CH6953755 inhibits YES1 kinase, leading to antitumor activity against YES1 Gene -amplified cancers in vitro and in vivo.

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CH6953755 Chemical Structure

CH6953755 Chemical Structure

CAS No. : 2055918-71-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 186 In-stock
Solution
10 mM * 1 mL in DMSO USD 186 In-stock
Solid
5 mg USD 153 In-stock
10 mg USD 246 In-stock
25 mg USD 468 In-stock
50 mg USD 750 In-stock
100 mg USD 1200 In-stock
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Based on 3 publication(s) in Google Scholar

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Description

CH6953755 is a potent, orally active and selective YES1 kinase (a member of the SRC family) inhibitor with an IC50 of 1.8 nM. CH6953755 inhibits YES1 kinase, leading to antitumor activity against YES1 Gene -amplified cancers in vitro and in vivo[1].

IC50 & Target

IC50: 1.8 nM (YES1)[1]
In Vitro

CH6953755 (0.001-1 μM; for 4 days) inhibits the cell growth of YES1-amplified cancer cell lines[1].
CH6953755 (0.001-1 μM; for 2 hours) prevents the autophosphorylation at Tyr426 of YES1 that upregulates enzymatic activity in KYSE70 cells harboring YES1 amplification[1].
CH6953755 (0.1, 0.3, 1, 3 μM) suppresses TEAD luciferase reporter activity in YES1-amplified KYSE70 and RERF-LC-AI[1].

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

CH6953755 Related Antibodies

Cell Viability Assay[1]

Cell Line: YES1-amplified cancer cell lines KYSE70 and OACP4 C, and non-YES1–amplified cancer cell line K562 expressing YES1-WT or YES1-GK
Concentration: 0.001, 0.01, 0.1, 1 μM
Incubation Time: 4 days
Result: Inhibited the cell growth of YES1-amplified cancer cell lines.

Western Blot Analysis[1]

Cell Line: KYSE70 cell line
Concentration: 0.001, 0.003, 0.01, 0.03, 0.1, 0.3, 1 μM
Incubation Time: 2 hours
Result: Prevented the autophosphorylation at Tyr426 of YES1 that upregulates enzymatic activity in KYSE70 cells harboring YES1 amplification
In Vivo

CH6953755 (oral; 60 mg/kg/day; for 10 days) shows selective antitumor activity accompanied with phospho-Tyr426 YES1 suppression in xenograft tumors[1].
CH6953755 (oral; 7.5, 15, 30, 60 mg/kg) suppresses phospho-Tyr426 YES1 in a dose-dependent manner[1].

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

Animal Model: Female BALB/c-nu/nu mice with Rat-2_YES1 xenograft[1]
Dosage: 60 mg/kg
Administration: Oral; daily; for 10 days
Result: Showed selective antitumor activity accompanied with phospho-Tyr426 YES1 suppression in xenograft tumors.
Molecular Weight

552.55

Formula

C26H22F2N6O4S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CS(=O)(NC1=CC2=C(C=C1C)C=C(C(C3=C(N)N(C4=C(C)C=C(OC5=C(F)C=CC=C5F)N=C4)N=C3)=O)N2)=O
Shipping

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

DMSO : 125 mg/mL (226.22 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 1.8098 mL 9.0490 mL 18.0979 mL
5 mM 0.3620 mL 1.8098 mL 3.6196 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.08 mg/mL (3.76 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (3.76 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:

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(per animal)

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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

Purity: 98.03%

COA (251 KB) LCMS (269 KB)

Handling Instructions (2659 KB)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8098 mL 9.0490 mL 18.0979 mL 45.2448 mL
5 mM 0.3620 mL 1.8098 mL 3.6196 mL 9.0490 mL
10 mM 0.1810 mL 0.9049 mL 1.8098 mL 4.5245 mL
15 mM 0.1207 mL 0.6033 mL 1.2065 mL 3.0163 mL
20 mM 0.0905 mL 0.4524 mL 0.9049 mL 2.2622 mL
25 mM 0.0724 mL 0.3620 mL 0.7239 mL 1.8098 mL
30 mM 0.0603 mL 0.3016 mL 0.6033 mL 1.5082 mL
40 mM 0.0452 mL 0.2262 mL 0.4524 mL 1.1311 mL
50 mM 0.0362 mL 0.1810 mL 0.3620 mL 0.9049 mL
60 mM 0.0302 mL 0.1508 mL 0.3016 mL 0.7541 mL
80 mM 0.0226 mL 0.1131 mL 0.2262 mL 0.5656 mL
100 mM 0.0181 mL 0.0905 mL 0.1810 mL 0.4524 mL
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CH6953755 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:

CH69537552055918-71-1CH 6953755CH-6953755SrcorallyYES1SRCfamilyantitumorGene-amplifiedcancersautophosphorylationTyr426phospho-Tyr426Inhibitorinhibitorinhibit

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