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).
For research use only. We do not sell to patients.
- Formula: C43H52ClN11O6
- Molecular Weight:854.40
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Storage:
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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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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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Molecular Weight 854.40
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ISM-PR44 Related Classifications
HY-189442 Related Classifications
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