製品番号: 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 96.20%
CAS 番号: 2884554-45-2
分子式: C₄₂H₄₄N₁₀O₄
分子量:752.86

保管条件:

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

UBX-382 構造式

CAS 番号: 2884554-45-2

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

Cereblon

PROTACs アイソフォーム固有の製品をすべて表示 :

MEK アイソフォーム固有の製品をすべて表示 :

ERK アイソフォーム固有の製品をすべて表示 :

体外実験

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.

体内実験

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.

化学情報

CAS 番号 2884554-45-2
性状 Solid
分子量 752.86
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (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)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

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

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希釈計算機

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濃度 _(開始) 濃度 _(開始)

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濃度 _(終了) 濃度 _(終了)

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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

PROTACs アイソフォーム固有の製品をすべて表示

MEK アイソフォーム固有の製品をすべて表示

ERK アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

UBX-382 関連分類

HY-160142 関連分類