Referencia número: HY-160142

UBX-382

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Based on 1 Customer Validation

UBX-382 is an orally active BTK PROTAC degrader with a DC₅₀ of 4.56 nM. UBX-382 inhibits B-cell receptor signaling by targeting BTK. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins. UBX-382 inhibits tumor growth in murine xenograft models harboring wild-type or C481S mutant BTK-expressing TMD-8 cells. UBX-382 can be used for the study of B-cell-related blood cancers.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 96.20%
No. CAS: 2884554-45-2
Fòrmula: C₄₂H₄₄N₁₀O₄
Peso molecular:752.86

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

UBX-382 Chemical Structure

No. CAS: 2884554-45-2

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

Cereblon

Ver todos los productos específicos de isoformas PROTACs :

Ver todos los productos específicos de isoformas MEK :

Ver todos los productos específicos de isoformas ERK :

In Vitro

UBX-382 (0.00001-10 nM, 0.5-48 h) induces potent BTK degradation with a DC ₅₀ of 4.56 nM in TMD-8 cells^[1].
UBX-382 (0.0001-10 μM, 3-5 days) inhibits the proliferation of TMD8 (IC₅₀ = 14 nM), WSU-DLCL2 (IC₅₀ = 18 nM), OCI-Ly3 (IC₅₀ = 199 nM) and U2932 (IC₅₀ = 21 nM) measured by the Cell Titer-Glo assay in duplicates^[1].
UBX-382 (10 nM, 24 h) significantly inhibits CCL3 and CCL4 secretion induced by BCR signal activation in TMD-8 cells^[1].
UBX-382 (100 nM, 6-24 h) inhibits the phosphorylation of BTK Y223, SYK, MEK, and ERK in U2932 cells^[1].
UBX-382 (0.1-10 μM, 24 h) effectively degrades wild-type and various BTK mutants (E41K, C481S/R/T/Y/F, L528W) in HEK293 cells and strongly suppresses their phosphorylation^[1].

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

Western Blot Analysis^[1]

Cell Line:

U2932 cells
Concentration:

100 nM
Incubation Time:

6, 24 h
Result:

Showed far more effective inhibition of BTK Y223 phosphorylation than Ibrutinib (HY-10997), Acalabrutinib (HY-17600), and Nemtabrutinib (ARQ-531) (HY-112215) in U2932 cells.
Inhibited the phosphorylation of SYK, MEK, and ERK.

In Vivo

UBX-382 (3-30 mg/kg, p.o., once daily, 21 days) inhibits the growth of tumor in TMD-8 xenograft models and TMD-8 BTK C481S xenograft model^[1].

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

Animal Model:

TMD-8 cells (1 × 10⁷ in Matrigel) were subcutaneously injected into the flanks of 6-week-old CB17/severe combined immunodeficient mice^[1]
Dosage:

3, 10, 30 mg/kg
Administration:

p.o. once daily for 21 days
Result:

Achieved complete tumor regression in TMD-8 xenograft models.
Showed no significant changes in body weight and no other clinical toxicity signs during the experiment.
Reduced BTK levels in tumors of TMD-8 xenograft models.

Animal Model:

TMD-8 BTK C481S cells were subcutaneously inoculated into the right flank of male CB17/severe combined immunodeficient mice^[1]
Dosage:

3, 10, 30 mg/kg
Administration:

p.o. once daily for 21 days
Result:

Induced remarkable dose-dependent tumor regression in TMD-8 BTK C481S xenograft models, while Ibrutinib failed to inhibit tumor growth.

Chemical Information

No. CAS 2884554-45-2
Appearance Solid
Peso molecular 752.86
Fòrmula C₄₂H₄₄N₁₀O₄
Color Light yellow to green yellow
SMILES

O=C1C2=CC=C(N3CCC(CC3)CN4CC5=CC(NC6=NC7=C(C(NC8=C(C)C=CC=C8C)=NN7C)C=N6)=CC=C5CC4)C=C2C(N1C9C(NC(CC9)=O)=O)=O
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (271 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Lim YS, et al. Orally bioavailable BTK PROTAC active against wild-type and C481 mutant BTKs in human lymphoma CDX mouse models. Blood Adv. 2023;7(1):92-105. [Content Brief]

Calculators

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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.

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UBX-382

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

PROTAC Library

Autoimmune Disease Compound Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Lactylation Compound Library

Ver todos los productos específicos de isoformas PROTACs

Ver todos los productos específicos de isoformas MEK

Ver todos los productos específicos de isoformas ERK

Actividad biológica

Chemical Information

Pureza y Documentación

Referencias

Calculators

Help & FAQs

UBX-382 Related Classifications

HY-160142 Related Classifications