ABBV-744

製品コードS8723 バッチS872301

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₈H₃₀FN₃O₄

分子量

491.55

CAS No.

2138861-99-9

Solubility (25°C)*

体外

DMSO

98 mg/mL (199.36 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	4.900mg/ml (9.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 98 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.615mg/ml (1.25mM)	Taking the 1 mL working solution as an example, add 50 μL of 12.3 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2, BRD3 and BRD4. It is developed for treating AML and cancers.
in vitro	ABBV-744 is a potent inhibitor specific for BDII of BRD2/3/4, with >250-fold differential binding preference for BDII over BDI and excellent drug-like properties. This compound is also a potent and selective inhibitor of the AR (androgen receptor) transcription pathway^[1].
in vivo	In vivo, doses of this compound at fractions of its maximum tolerated dose (MTD) induces tumor growth inhibition in AML and prostate cancer xenograft models that were comparable to those observed with ABBV-075 when dosed at its MTD^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Cell-free assays
	濃度	IC50: 8, 13, 18, and 4 nM for BRD2, BRD3, BRDT, and BRD4.
	反応時間
	実験の流れ
動物実験	動物モデル	Male Sprague-Dawley (SD) rats
	投薬量	60 mg/kg
	投与方法	o.g.

参考

http://cancerres.aacrjournals.org/content/78/13_Supplement/4960
https://pubmed.ncbi.nlm.nih.gov/31969702/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Synergistic Sensitization of High-Grade Serous Ovarian Cancer Cells Lacking Caspase-8 Expression to Chemotherapeutics Using Combinations of Small-Molecule BRD4 and CDK9 Inhibitors [ Cancers (Basel), 2023, 16(1)107]	PubMed: 38201534
Selective BD2 Inhibitor Exerts Anti-Fibrotic Effects via BRD4/FoxM1/Plk1 Axis in Orbital Fibroblasts From Patients With Thyroid Eye Disease [ Invest Ophthalmol Vis Sci, 2023, 64(7):9]	PubMed: 37272763
BRD2 inhibition blocks SARS-CoV-2 infection by reducing transcription of the host cell receptor ACE2 [ Nat Cell Biol, 2022, 24(1):24-34]	PubMed: 35027731
Viral E protein neutralizes BET protein-mediated post-entry antagonism of SARS-CoV-2 [ Cell Rep, 2022, 40(3):111088]	PubMed: 35839775
Breaking boundaries: Pan BETi disrupt 3D chromatin structure, BD2-selective BETi are strictly epigenetic transcriptional regulators [ Biomed Pharmacother, 2022, 152:113230]	PubMed: 35687908
Targeting CCR2+ macrophages with BET inhibitor overcomes adaptive resistance to anti-VEGF therapy in ovarian cancer [ J Cancer Res Clin Oncol, 2022, 148(4):803-821]	PubMed: 35094142
Targeting CCR2+ macrophages with BET inhibitor overcomes adaptive resistance to anti-VEGF therapy in ovarian cancer [ J Cancer Res Clin Oncol, 2022, 10.1007/s00432-021-03885-z]	PubMed: 35094142
PDI inhibitor LTI6426 enhances panobinostat efficacy in preclinical models of multiple myeloma [ Cancer Chemother Pharmacol, 2022, 89(5):643-653]	PubMed: 35381875
BRD2 inhibition blocks SARS-CoV-2 infection in vitro by reducing transcription of the host cell receptor ACE2 [ bioRxiv, 2021, 2021.01.19.427194]	PubMed: 33501440
Viral E Protein Neutralizes BET Protein-Mediated Post-Entry Antagonism of SARS-CoV-2 [ bioRxiv, 2021, 2021.11.14.468537]	PubMed: 34816261

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。