KT-333
Based on 1 Customer Validation
KT-333 is a molecular glues that degrades STAT3 protein. KT-333 mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.91%
- No. CAS: 2502186-79-8
- Fòrmula: C60H74ClN10O14PS
- Peso molecular:1257.78
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Almacenamiento:Powder -20°C, 3 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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
STAT3 |
In Vitro
KT-333 (11.8±2.3 nM, 48 h) degrades STAT3 resulted in irreversible growth inhibition of SU-DHL-1 cell line and induces caspase 3/7 activity in the SU-DHL-1 cell line[1].
KT-333 has a good degradation effect on STAT3 protein, and in cell phenotypic analysis, its GI50 value in multiple ALCL cell lines ranges from 8.1 to 57.4 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
KT-333 (10, 20 and 30 mg/kg, iv.; once a week for two weeks) exhibits dose-dependent antitumor activity. Female NOD SCID mice with xenograft tumors of SUP-M2 administered with 10 mg/kg achieved 83.8% tumor growth inhibition (TGI), while those administered 20 or 30 mg/kg experienced complete tumor regression, with these effects sustained until the end of the study[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2502186-79-8
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Appearance Solid
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Peso molecular 1257.78
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Fòrmula C60H74ClN10O14PS
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Color White to off-white
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SMILES
O=C([C@H]1N(C([C@H](C2)NC(C3=CC4=CC(C([P](O)(O)=O)=O)=CC=C4N3)=O)=O)[C@](CCN2C(C)=O)([H])CC1)N[C@@H](CCC(N)=O)COC(C=CC=C5CCCC(N[C@@H](C(C)(C)C)C(N(C[C@@H]6O)[C@@H](C6)C(N[C@H](C7=CC=C(C(SC=N8)=C8C)C=C7)C)=O)=O)=O)=C5Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 116.67 mg/mL (92.76 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)
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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, 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 | 0.7951 mL | 3.9753 mL | 7.9505 mL | 19.8763 mL |
| 5 mM | 0.1590 mL | 0.7951 mL | 1.5901 mL | 3.9753 mL | |
| 10 mM | 0.0795 mL | 0.3975 mL | 0.7951 mL | 1.9876 mL | |
| 15 mM | 0.0530 mL | 0.2650 mL | 0.5300 mL | 1.3251 mL | |
| 20 mM | 0.0398 mL | 0.1988 mL | 0.3975 mL | 0.9938 mL | |
| 25 mM | 0.0318 mL | 0.1590 mL | 0.3180 mL | 0.7951 mL | |
| 30 mM | 0.0265 mL | 0.1325 mL | 0.2650 mL | 0.6625 mL | |
| 40 mM | 0.0199 mL | 0.0994 mL | 0.1988 mL | 0.4969 mL | |
| 50 mM | 0.0159 mL | 0.0795 mL | 0.1590 mL | 0.3975 mL | |
| 60 mM | 0.0133 mL | 0.0663 mL | 0.1325 mL | 0.3313 mL | |
| 80 mM | 0.0099 mL | 0.0497 mL | 0.0994 mL | 0.2485 mL |
KT-333 Related Classifications
HY-156730 Related Classifications
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