(R)-Zelebrudomide
Based on 1 Customer Validation
(R)-Zelebrudomide ((R)-NX-2127) is an isomer of Zelebrudomide (HY-153220). Zelebrudomide is an orally active BTK-targeting PROTAC degrader, with DC50 values of 4.5 nM and 31 nM against wild-type BTK and BTKC481S mutant, respectively. Zelebrudomide recruits the cereblon E3 ubiquitin ligase complex to mediate the degradation of BTK. Zelebrudomide also acts as a molecular glue to bind the cereblon E3 ubiquitin ligase complex, mediating the degradation of IKZF1 and IKZF3. Zelebrudomide can be used in the research of B-cell malignancies.
(Pink: Btk ligand (HY-168302); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-168348)).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.93%
- CAS. Nr.: 3024312-52-2
- Formel: C39H45N9O5
- Molecular Weight:719.83
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Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Alle PROTACs Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
|
IKZF1 57 nM (DC50) |
IKZF3 36 nM (DC50) |
IL-2 |
(R)-Zelebrudomide ((R)-NX-2127) is an isomer of Zelebrudomide (HY-153220). Zelebrudomide (NX-2127) degrades wild-type BTK in TMD8 cells with a DC50 of 4.5 nM; it also degrades the BTKC481S mutant with a DC50 of 31 nM[1].
(R)-Zelebrudomide is an isomer of Zelebrudomide. Zelebrudomide (50 nM; 4 h) selectively degrades BTK in human peripheral blood mononuclear cells (PBMCs) from normal donors[1].
(R)-Zelebrudomide is an isomer of Zelebrudomide. Zelebrudomide (0.001-100 nM; 1-24 h) degrades IKZF1 (DC50 = 57 nM) and IKZF3 (DC50 = 36 nM) in primary human T cells, and induces IL-2 secretion in TCR-activated primary human T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
(R)-Zelebrudomide is an isomer of Zelebrudomide. Zelebrudomide (10-100 mg/kg; p.o.; single dose, once daily for 14 consecutive days) induces potent, dose-dependent degradation of BTK and IKZF3 in cynomolgus monkeys[1].
(R)-Zelebrudomide is an isomer of Zelebrudomide. Zelebrudomide (10-90 mg/kg; p.o.; daily administration for 5 consecutive days, daily administration for 25 consecutive days) induces dose-dependent anti-tumor efficacy in TMD8 BTKWT xenograft tumors and degrades BTK, IKZF1 and IKZF3[1].
(R)-Zelebrudomide is an isomer of Zelebrudomide. Zelebrudomide (10-90 mg/kg; p.o.; daily administration for 25 days) exerts dose-dependent antitumor efficacy in Ibrutinib (HY-10997)-resistant TMD8 BTKC481S xenograft tumors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 3024312-52-2
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Appearance Solid
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Molecular Weight 719.83
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Formel C39H45N9O5
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Color Light yellow to yellow
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SMILES
O=C1C2=CC(N3C[C@@H](CN4CCC(C5=CC=C(C=C5)NC6=C(N=CC(N7CCCCC7)=N6)C(N)=O)CC4)CC3)=CC=C2C(N1C8C(NC(CC8)=O)=O)=O
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Synonyms
(R)-NX-2127
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Reinheit & Dokumentation
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
(R)-Zelebrudomide Related Classifications
HY-153220A Related Classifications
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