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Art. -Nr.: HY-189441

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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 CRL4^CRBN 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).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₅₀H₅₉N₁₁O₆
Molecular Weight:910.07

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

ISM-PR25 Chemical Structure

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Preis

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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 CRL4^CRBN E3 ligase-mediated ubiquitination. ISM-PR25 can be used for research on B-cell lymphoma^[1]. (Pink: Btk ligand (HY-170324); Blue: Cereblon E3 ligase ligand; Black: linker).

IC₅₀ & Target

^[1]

BTK

0.04 nM (DC₅₀)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

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	AUC_0-t	C_max	T_1/2	F
Mice^[1]	1 mg/kg	i.v.	18119 ng·h/mL	3903 ng/mL	2.0 h	26 %

In Vivo

ISM-PR25 (compound 25) (3 mg/kg; p.o.; single administration) effectively degrades BTK in mouse circulating B cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/c nude mice (female, 6-8 weeks)^[1]
Dosage:

3 mg/kg
Administration:

p.o.; single dose
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

Molecular Weight 910.07
Formel C₅₀H₅₉N₁₁O₆
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Mantsyzov AB, et al. Discovery of Highly Potent and Selective, Orally Bioavailable BTK-Targeting PROTACs Featuring Novel CRBN-Binding Warheads. Journal of medicinal chemistry. 2026 Sep 10;69(17):20494-20519. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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