YSA64
Based on 1 Customer Validation
YSA64 is an orally active RBM39-targeting molecular glue. YSA64 promotes degradation via formation of a DCAF15/DDB1 ternary complex, dependent on Cullin-RING E3 ligase and proteasome activity. YSA64 can be used for the research of acute myeloid leukemia and Ewing sarcoma.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 98.06%
- Formule: C25H24N4O3S
- Masse moléculaire:460.55
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
YSA64 (Compound 41) (4 days) potently inhibits HCT-116 colorectal cancer cell proliferation with an IC50 of 166 nM[1].
YSA64 (0.05-0.8 μM; 24 h) induces robust degradation of RBM39 in HCT-116 colorectal cancer cells[1].
YSA64 (4 days) inhibits proliferation of multiple cancer cell lines with varying potency, showing highest activity in A673 Ewing sarcoma (IC50 = 125.3 nM) and MV4-11 acute myeloid leukemia (IC50 = 111.7 nM) cells[1].
YSA64 (24 h) induces robust degradation of RBM39 and CEP192 in A673 Ewing sarcoma cells[1].
YSA64-induced RBM39 degradation in A673 Ewing sarcoma cells requires intact proteasome and Cullin-RING E3 ligase activity[1].
YSA64 (24 h) induces dose-dependent degradation of RBM39 and CEP192 in MV4-11 acute myeloid leukemia cells following 24 h incubation, with RBM39 degradation potency comparable to E7820[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116 colorectal cancer cells
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Concentration:0.05 μM; 0.2 μM; 0.8 μM
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Incubation Time:24 h
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Result:Robustly reduced RBM39 protein levels at all tested concentrations.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID mice (male; 3-4 weeks old; subcutaneously implanted with MV4-11 cells to establish a xenograft model)[1]
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Dosage:100 mg/kg; 150 mg/kg; 200 mg/kg
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Administration:p.o.; once daily; 10 days
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Result:Achieved a tumor growth inhibition (TGI) value of 51.9% at 200 mg/kg.
Yielded unspecified tumor inhibition at 100 mg/kg.
Achieved a tumor growth inhibition rate of 44.1% at 150 mg/kg.
Caused no overt toxicity or weight loss at any tested dose.
Chemical Information
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Appearance Solid
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Masse moléculaire 460.55
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Formule C25H24N4O3S
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Color White to off-white
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SMILES
CNC1=CC=C(C(COC)=C1)C2=CC=CC(S(=O)(NC3=C4NC=C(C4=C(C=C3)C)C#N)=O)=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 20 mg/mL (43.43 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, 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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 2.1713 mL | 10.8566 mL | 21.7132 mL | 54.2829 mL |
| 5 mM | 0.4343 mL | 2.1713 mL | 4.3426 mL | 10.8566 mL | |
| 10 mM | 0.2171 mL | 1.0857 mL | 2.1713 mL | 5.4283 mL | |
| 15 mM | 0.1448 mL | 0.7238 mL | 1.4475 mL | 3.6189 mL | |
| 20 mM | 0.1086 mL | 0.5428 mL | 1.0857 mL | 2.7141 mL | |
| 25 mM | 0.0869 mL | 0.4343 mL | 0.8685 mL | 2.1713 mL | |
| 30 mM | 0.0724 mL | 0.3619 mL | 0.7238 mL | 1.8094 mL | |
| 40 mM | 0.0543 mL | 0.2714 mL | 0.5428 mL | 1.3571 mL |
YSA64 Related Classifications
HY-183755 Related Classifications
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