GLPBio

BET bromodomain inhibitor

Catalog No.: GC16299Purity:>99.50%Synonyms: CPI-0610; CPI0610; CPI 0610
COASDSData Sheet
BET ブロモドメイン阻害剤は、特許 WO/2015/153871A2、化合物例 11 から抽出された強力な BET 阻害剤です。

製品は研究用途にのみ使用できます。人体には使用できません。患者への販売は行っておりません。

BET bromodomain inhibitor
Cas No.: 1380087-89-7
10mM (in 1mL DMSO)In Stock
$97.00
1
10mgIn Stock
$162.00
1
50mgIn Stock
$558.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

引用文献 (Citations)

現在、この製品の引用文献はありません。以下はGlpBio製品を引用した代表的な文献です。
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    641, 529–536 (2025)
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    Nature
    632, 686–694 (2024)
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    618, 1017–1023 (2023)
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    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
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    Science
    388(6745) (2025)
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    Science
    387(6734) (2025)
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    Cell Research
    35, 97–116 (2025)
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    34, 683–706 (2024)
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    31, 1291–1307 (2021)

製品説明 (Description)

IC50: < 500 nM for BRD4

BET (bromodomain and extra-terminal) proteins regulate gene expression through their ability to bind to acetylated chromatin and subsequently activate RNA PolII-driven transcriptional elongation. The bromodomain (BRD) and extra-C terminal domain (BET) protein family consists of four members (BRD2, BRD3, BRD4 and BRDT).Small molecule BET inhibitors prevent binding of BET proteins to acetylated histones and inhibit transcriptional activation of BET target genes. BET inhibitors attenuate cell growth and survival in several hematologic cancer models, partially through the down-regulation of the critical oncogene, MYC. BET bromodomain inhibitor is a potent and selective inhibitor for BRD4.

In vitro: The most potent systhsized ompound presented is BET bromodomain inhibitor, which shows activity with IC50 < 500 nM against BRD4 [1].

In vivo: BET bromodomain inhibitor shows activity in vivo at < 10 mg/kg against BRD4 in rat [1].

Clinical trial: Up to now, BET bromodomain inhibitor is still in the preclinical development stage.

Reference:
[1] Garnier JM, Sharp PP, Burns CJ.  BET bromodomain inhibitors: a patent review. Expert Opin Ther Pat. 2014 Feb;24(2):185-99.

実験プロトコル (Protocol)

Cell experiment [1]:

Cell lines

Primary Multiple Myeloma cell lines

Preparation method

The solubility of this compound in DMSO is >18.3mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

2 μM at 72 h

Applications

CPI-0610 treatment resulted in 40% decrease in viability in primary cells isolated from a newly diagnosed patient and caused 50% cell death in primary cells isolated from a relapsed disease patient.
Animal experiment [1]:

Animal models

Multiple Myeloma xenograft CB17-SCID mouse model

Dosage form

subcutaneous injections, 10 mg/kg, twice a day for 38 days

Application

Mice treated with CPI-0610 showed a significant delay in tumor growth, and the median overall survival of CPI-0610 treated animals was significantly prolonged.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Siu KT, Ramachandran J, Yee AJ, et al. Preclinical activity of CPI-0610, a novel small-molecule bromodomain and extra-terminal protein inhibitor in the therapy of multiple myeloma. Leukemia. 2017 Jan 3.

製品資料 (Product Documents)

Purity:>99.50%Appearance:A solid
COASDSData Sheet

化学的性質 (Chemical Properties)

CAS番号
1380087-89-7
同義語
CPI-0610; CPI0610; CPI 0610
化学名
2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetimidic acid
SMILES
CC1=NOC2=C1C3=CC=CC=C3C(C4=CC=C(Cl)C=C4)=N[C@@]2([H])CC(O)=N
分子式
C20H16ClN3O2
分子量
365.81
溶解性
≥ 18.3mg/mL in DMSO
保存条件
Store at -20°C
一般的な注意事項
製品の溶解性データに基づいて適切な溶媒を選択してください。調製後は、凍結融解の繰り返しを避けるため、ストック溶液を小分けしてください。
ストック溶液は、-80°Cで保存する場合は6か月以内、-20°Cで保存する場合は1か月以内に使用してください。
溶解性を高めるには、チューブを37°Cに温め、適切な時間超音波処理してください。
配送条件
評価用サンプルは保冷剤とともに発送します。その他の容量は室温で発送し、ご要望に応じて保冷剤を同梱します。

計算ツール (Calculators)モル濃度 / 希釈 / 分子量 / 単位変換 / in vivo製剤 / 溶解度

g/mol

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