ISM-PR25
ISM-PR25 is an orally active PROTAC degrader targeting BTK, with a DC50 of 0.04 nM in Ramos cells. ISM-PR25 degrades BTK protein via CRL4CRBN E3 ligase-mediated ubiquitination. ISM-PR25 can be used for research on B-cell lymphoma.
(Pink: Btk ligand (HY-170324); Blue: Cereblon E3 ligase ligand; Black: linker).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C50H59N11O6
- Masse moléculaire:910.07
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Stockage:
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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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
BTK 0.04 nM (DC50) |
In Vitro
ISM-PR25 (compound 25) (4 h) degrades BTK in Ramos cells with a DC50 of 0.04 nM[1].
ISM-PR25 (120 h) inhibits the viability of TMD8 cells expressing wild-type and mutant BTK, with IC50 values of 5.6, 2.5, 9.0, and 10 nM, respectively[1].
ISM-PR25 binds to CRBN with an IC50 of 93 nM[1].
ISM-PR25 (7 days) shows a CTG HSC IC50 of 398 nM in human CD34+ hematopoietic stem cells[1].
ISM-PR25 (0.41 nM; 15 min) induces BTK/CRBN/PROTAC ternary complex formation with an EC50 of 0.41 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
Parmacokinetics
| Species | Dose | Route | AUC0-t | Cmax | T1/2 | F |
|---|---|---|---|---|---|---|
| Mice[1] | 1 mg/kg | i.v. | 18119 ng·h/mL | 3903 ng/mL | 2.0 h | 26 % |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (female, 6-8 weeks)[1]
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Dosage:3 mg/kg
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Administration:p.o.; single dose
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Result:Demonstrated a significant reduction of the BTK concentration in B-cells.
Showed comparable BTK degradation at both 2 h and 24 h, with efficacy at 24 h comparable to the reference NX-5948.
Chemical Information
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Masse moléculaire 910.07
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Formule C50H59N11O6
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SMILES
O=C(C1=NC=C(N2C[C@H](N3CCN(C)C3=O)CCC2)N=C1NC4=CC=C(C5CCN(CC6=CC=C(CN([C@@]7(C)C(N([C@@H](CC8)C(NC8=O)=O)CC7)=O)C(C9=CC=CC=C9)=O)C=C6)CC5)C=C4)N
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ISM-PR25 Related Classifications
HY-189441 Related Classifications
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