CSI86
CSI86 is a c-MYC PROTAC degrader. CSI86 inhibits the proliferation of various cancer cells and exhibits excellent cellular uptake capacity. CSI86 maintains stability for 72 h in cell culture medium. CSI86 can be used in studies related to breast cancer and prostate cancer.
(Pink: MYC ligand (HY-169379); Blue: VHL ligand (HY-120217); Black: linker (HY-79369)).
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- Fòrmula: C48H50F9N7O7S
- Peso molecular:1040.00
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
Descripciòn
In Vitro
CSI86 (200 μM) directly binds to recombinant bHLH-MYC protein at a concentration of 200 μM[1].
CSI86 (150 μM; 10 min) does not significantly interfere with the formation of the MYC-MAX complex in recombinant protein pull-down assays[1].
The cellular uptake rate of CSI86 (10 μM; 24 h) reaches 26% in SKBR3 cells, 19% in PC3 cells, and 10% in A549 cells[1].
CSI86 (0.1-100 μM; 72 h) inhibits the growth of SKBR3 human breast cancer cells and PC3 human prostate adenocarcinoma cells, with IC50 values of 15 μM and 18 μM, respectively; it shows no activity against A549 human lung adenocarcinoma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC3 human prostate adenocarcinoma cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Reduced c-MYC protein levels relative to untreated control cells.
Parmacokinetics
| Species | Dose | Route | Cmax | AUC0-24 | Tmax | T1/2 |
|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 713 ng/mL | 8.4 μg·h/mL | 2 h | 7.4 h |
Chemical Information
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Peso molecular 1040.00
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Fòrmula C48H50F9N7O7S
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SMILES
CC1=C(SC=N1)C2=CC=C(C=C2)CNC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(CCC(NCCCOC4=C(C(O)=C(C=C4)C5=CC(C(F)(F)F)=NN5C)C6=CC(C(F)(F)F)=CC(C(F)(F)F)=C6)=O)=O)=O)O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CSI86 Related Classifications
HY-169378 Related Classifications
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