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  3. BETd-246

BETd-246 

目录号: HY-115568
产品使用指南

BETd-246 是第二代 BET溴端结构域 (BRD) 的抑制剂,具有良好的选择性、有效性和抗肿瘤活性。

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BETd-246 Chemical Structure

BETd-246 Chemical Structure

CAS No. : 2140289-17-2

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Description

BETd-246 is a second-generation BET bromodomain (BRD) inhibitor, exhibiting superior selectivity, potency and antitumor activity[1].

IC50 & Target

BET BRD[1].

In Vitro

BETd-246 treatment (0-100 nM, 1-3 h) causes a dose-dependent depletion of BRD2, BRD3 and BRD4 in representative TNBC cell lines with 30-100 nM for 1 h or with 10-30 nM for 3 h incubation.
BETd-246 (100 nM, 24/48 hours) displays strong growth inhibition and apoptosis induction activity in MDA-MB-468 cell lines. BETd-246 induces a rapid and time-dependent downregulation of MCL1 protein in all the TNBC cell lines evaluated. BETd-246 induces much stronger apoptosis than BETi-211.
BETd-246 (100 nM, 24 hours) induces pronounced cell cycle arrest and apoptosis in TNBC cell lines[1].

Cell Proliferation Assay[1]

Cell Line: MDA-MB-468 cells
Concentration: 100 nM
Incubation Time: 24 or 48 hours
Result: Displayed strong growth inhibition and apoptosis induction activity in TNBC cell lines.

Cell Cycle Analysis[1]

Cell Line: Human TNBC cells
Concentration: 100 nM
Incubation Time: 24 hours
Result: Induced pronounced cell cycle arrest and apoptosis in TNBC cell lines.

Western Blot Analysis[1]

Cell Line: Human TNBC cells
Concentration: 0-100 nM
Incubation Time: 1-3 hours
Result: Caused a dose-dependent depletion of BRD2, BRD3 and BRD4.
In Vivo

BETd-246 (5 mg/kg, IV, 3 times per week for 3 weeks) treatment effectively inhibits WHIM24 tumor growth, similar to the antitumor activity of BETi-211 with higher dosage and more frequently administration. The treatment of 10 mg/kg induces partial tumor regression during treatment without apparent toxicity. BETd-246 has very limited drug exposure in the xenograft tumor tissue in MDA-M-231and MDA-MB-468 models[1].

Animal Model: “Washington Human in Mouse (WHIM)” (PDX) model developed from a patient with treatment-resistant breast cancer (ESRE380Q, PR- and HER2-))[1].
Dosage: 5, 10 mg/kg
Administration: IV, 3 times per week for 3 weeks.
Result: Effectively inhibited WHIM24 tumor growth.
Storage

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

References
Molecular Weight

946.02

Formula

C₄₈H₅₅N₁₁O₁₀

CAS No.

2140289-17-2

SMILES

O=C(C1=NC(NC2=CC(C3CC3)=NN2CC)=C4C(NC5=C4C=C(OC)C(C6=C(C)ON=C6C)=C5)=N1)NCCCOCCOCCOCCCNC7=CC=CC(C(N8C(CC9)C(NC9=O)=O)=O)=C7C8=O

Shipping

Room temperature in continental US; may vary elsewhere

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产品名称:
BETd-246
目录号:
HY-115568
需求量:

BETd-246

Cat. No.: HY-115568