Shanghai Nianxing Industrial Co., Ltd
China
Product Name: BETd-246?
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Purity: 98.0%
Stocking Period: 10 Day
Contact: Huang

ShangHai DC Chemicals Co.,Ltd
China
Product Name: BETd-246
Price: ￥Inquiry/1g
Purity: 98.9%
Stocking Period: 1 Day
Contact: Tony Lai

DC Chemicals Limited
China
Product Name: BETd-246
Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

2140289-17-2

2140289-17-2 structure

2140289-17-2 structure

Name: BETd-246
Chemical Name: BETd-246
CAS Number: 2140289-17-2
Molecular Formula: C₄₈H₅₅N₁₁O₁₀
Molecular Weight: 946.02
Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
Create Date: 2019-03-30 17:49:34
Modify Date: 2024-01-08 09:34:34
BETd-246 is a second-generation BET bromodomain (BRD) inhibitor, exhibiting superior selectivity, potency and antitumor activity[1].

Name	BETd-246

Description	BETd-246 is a second-generation BET bromodomain (BRD) inhibitor, exhibiting superior selectivity, potency and antitumor activity[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain
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.
References	[1]. Bai L, et al. Targeted Degradation of BET Proteins in Triple-Negative Breast Cancer. Cancer Res. 2017 May 1;77(9):2476-2487.

Molecular Formula	C₄₈H₅₅N₁₁O₁₀
Molecular Weight	946.02
Storage condition	2-8℃