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製品番号: HY-122703

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BETi-211

BETi-211 is an orally active, selective BET inhibitor with a K_i < 1 nM. BETi-211 inhibits BET function as epigenetic readers by binding to BET proteins (BRD2, BRD3, and BRD4). BETi-211 suppresses the growth of various triple-negative breast cancer (TNBC) cell lines, with an IC₅₀ < 1 μM. BETi-211 can be utilized to synthesize PROTAC molecules designed to degrade BET proteins. BETi-211 is applicable for research into TNBC.

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。

CAS 番号: 1995867-02-1
分子式: C₂₆H₂₉N₇O₃
分子量:487.55

保管条件:

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

Data Sheet (293 KB)

BETi-211 構造式

CAS 番号: 1995867-02-1

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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]

BET

< 1 nM (Ki)

BRD2

BRD4

BRD3

Epigenetic Reader Domain アイソフォーム固有の製品をすべて表示 :

体外実験

Anti-cancerCell Cycle RegulationApoptosisOthers

Anti-cancer

BETi-211 (4 days) inhibits the growth of TNBC cell lines, with an IC₅₀ <1 µM in 9 out of 13 cell lines^[1].
BETi-211 (1 µM; 3-8 h) upregulates the mRNA and protein expression of BRD2 and MCL1 in TNBC cell lines (MDA-MB-231, MDA-MB-468).^[1].

Anti-cancer

Cell Cycle Regulation

Apoptosis

BETi-211 (1 µM; 24-48 h) induces cell cycle arrest (with a reduction in S-phase cells) and moderate apoptosis in TNBC cell lines (such as MDA-MB-468)^[1].

Others

In biochemical assays, BETi-211 binds to BET proteins with a K_i <1 nM^[1].

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

Western Blot Analysis^[1]

Cell Line:

MDA-MB-468 and TNBC cell lines
Concentration:

1 µM
Incubation Time:

1 h, 3 h, 8 h
Result:

Did not degrade BET proteins but upregulated BRD2 and MCL1.

Real Time qPCR^[1]

Cell Line:

MDA-MB-157, MDA-MB-231, MDA-MB-468 cells
Concentration:

1 µM
Incubation Time:

3, 8 h
Result:

Caused mixed up- and down-regulation of genes.

Apoptosis Analysis^[1]

Cell Line:

MDA-MB-468 cells
Concentration:

1 µM
Incubation Time:

48 h
Result:

Elicited only modest apoptosis induction.

体内実験

Anti-cancer

BETi-211 (50 mg/kg; p.o.; once daily, 5 days per week; 2-3 weeks) inhibits tumor growth in SCID mouse models bearing human triple-negative breast cancer (TNBC) xenografts (WHIM24 PDX, MDA-MB-453, MDA-MB-231, and MDA-MB-468)^[1].

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

Animal Model:

SCID mice were injected subcutaneously with WHIM24 PDX, MDA-MB-453, MDA-MB-231, and MDA-MB-468 cells^[1]
Dosage:

50 mg/kg
Administration:

p.o.; once daily, 5 days per week; 2, 3 weeks
Result:

Effectively suppressed breast tumor growth at well-tolerated dosing schedules.
Did not cause significant weight loss or apparent toxicity in the mice.

Related Protocols :

Breast Cancer Modeling

化学情報

CAS 番号 1995867-02-1
分子量 487.55
分子式 C₂₆H₂₉N₇O₃
SMILES

COCC1=NC(NC2=CC(C3CC3)=NN2CC)=C4C(NC5=C4C=C(OC)C(C6=C(C)ON=C6C)=C5)=N1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

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 (293 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]. Bai L, et al. Targeted degradation of BET proteins in triple-negative breast cancer. Cancer research. 2017 May 1;77(9):2476-87.

Calculators

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Other size

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Amount: USD 0.00

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

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BETi-211

Epigenetic Reader Domain アイソフォーム固有の製品をすべて表示

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

BETi-211 関連分類

HY-122703 関連分類

Bioz

Keywords

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