Art. -Nr.: HY-160142

UBX-382

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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.

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Reinheit: 96.20%
CAS. Nr.: 2884554-45-2
Formel: C₄₂H₄₄N₁₀O₄
Molecular Weight:752.86

Speicherung:

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

UBX-382 Chemical Structure

CAS. Nr.: 2884554-45-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Cereblon

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle MEK Isoform-spezifische Produkte anzeigen :

Alle ERK Isoform-spezifische Produkte anzeigen :

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

CAS. Nr. 2884554-45-2
Appearance Solid
Molecular Weight 752.86
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (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)
Handling Instructions (2659 KB)

Verweise

[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

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.

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UBX-382

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Multi-Target Compound Library

Bioactive Compound Library Max

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle MEK Isoform-spezifische Produkte anzeigen

Alle ERK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

UBX-382 Related Classifications

HY-160142 Related Classifications