CH6953755
Based on 5 publication(s) in Google Scholar
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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- Pureza: 99.75%
- No. CAS: 2055918-71-1
- Fòrmula: C26H22F2N6O4S
- Peso molecular:552.55
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) CH6953755
More
Actividad biológica
IC50: 1.8 nM (YES1)[1]
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.
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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
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Concentration:0.001, 0.01, 0.1, 1 μM
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Incubation Time:4 days
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Result:Inhibited the cell growth of YES1-amplified cancer cell lines.
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Cell Line:KYSE70 cell line
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Concentration:0.001, 0.003, 0.01, 0.03, 0.1, 0.3, 1 μM
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Incubation Time:2 hours
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Result:Prevented the autophosphorylation at Tyr426 of YES1 that upregulates enzymatic activity in KYSE70 cells harboring YES1 amplification
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.
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Animal Model:Female BALB/c-nu/nu mice with Rat-2_YES1 xenograft[1]
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Dosage:60 mg/kg
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Administration:Oral; daily; for 10 days
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Result:Showed selective antitumor activity accompanied with phospho-Tyr426 YES1 suppression in xenograft tumors.
Chemical Information
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No. CAS 2055918-71-1
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Appearance Solid
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Peso molecular 552.55
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Fòrmula C26H22F2N6O4S
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Color Off-white to light yellow
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Cancer Res
Targeting YES1 Disrupts Mitotic Fidelity and Potentiates the Response to Taxanes in Triple-Negative Breast Cancer. [Abstract]2024 Nov 4;84(21):3556-3573. PMID: 39037997 -
Sci Adv
FeaSion decodes the regulatory landscape and functional diversity of RNA polymerase II CTD phosphorylation. [Abstract]2025 Nov 28;11(48):eadz2345. PMID: 41313762 -
Front Pharmacol
2021 Mar 8;12:644342. PMID: 33790797 -
bioRxiv
A Hotspot Phosphorylation Site on SHP2 Drives Oncoprotein Activation and Drug Resistance. [Abstract]2025 Jun 16:2025.06.11.659120. PMID: 40667115 -
Solvente y solubilidad
DMSO : 100 mg/mL (180.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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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