ISM-PR44
ISM-PR44 is an orally active PROTAC degrader targeting BTK, with a DC50 of 0.05 nM in BTK-HiBiT Ramos cells. ISM-PR44 recruits CRBN E3 ligase to induce ubiquitination and proteasomal degradation of BTK. ISM-PR44 exhibits antiproliferative and cytotoxic activities in B-cell lymphoma cells. ISM-PR44 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: C43H52ClN11O6
- Masse moléculaire:854.40
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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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
BTK 0.05 nM (DC50) |
In Vitro
ISM-PR44 (compound 44) (1 mM; 4 h) potently degrades BTK in BTK-HiBiT Ramos cells with a DC50 of 0.05 nM[1].
ISM-PR44 (30 μM; 15-60 min) exhibits potent binding to CRBN with an IC50 of 16 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | AUC0-t | Cmax | T1/2 |
|---|---|---|---|---|---|
| Mice[1] | 1 mg/kg | i.v. | 7991 ng·h/mL | 1693 ng/mL | 1.2 h |
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 comparable BTK degradation at both 2 h and 24 h postdose.
Chemical Information
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Masse moléculaire 854.40
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Formule C43H52ClN11O6
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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=CC(C(N[C@@]7(C)C(N([C@@H](CC8)C(NC8=O)=O)CC7)=O)=O)=C6Cl)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.
Protocole
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ISM-PR44 Related Classifications
HY-189442 Related Classifications
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