- 阻害剤
- 研究分野別
- PI3K/Akt/mTOR
- Epigenetics
- Methylation
- Immunology & Inflammation
- Protein Tyrosine Kinase
- Angiogenesis
- Apoptosis
- Autophagy
- ER stress & UPR
- JAK/STAT
- MAPK
- Cytoskeletal Signaling
- Cell Cycle
- TGF-beta/Smad
- 化合物ライブラリー
- FDA-approved Drug Library
- FDA-approved & Passed Phase I Drug Library
- Preclinical/Clinical Compound Library
- Bioactive Compound Library-I
- Bioactive Compound Library-II
- Kinase Inhibitor Library
- Express-Pick Library
- Natural Product Library
- Human Endogenous Metabolite Compound Library
- Covalent Inhibitor Library
- FDA-approved Anticancer Drug LibraryNew
- Highly Selective Inhibitor Library
- HTS Library for Drug Discovery
- Metabolism Compound Library
- 抗体
- 新製品
- お問い合わせ
INCB054329
INCB054329 is a structurally distinct bromodomain and extraterminal domain (BET) inhibitor with IC50 values of 44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM and 63 nM for BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2, respectively.
CAS No. 1628607-64-6
文献中Selleckの製品使用例（6）
INCB054329関連製品
シグナル伝達経路
Epigenetic Reader Domain阻害剤の選択性比較
1. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation. 2. "✔" indicates inhibitory effect, but without specific value.
生物活性
| 製品説明 | INCB054329 is a structurally distinct bromodomain and extraterminal domain (BET) inhibitor with IC50 values of 44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM and 63 nM for BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2, respectively. | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Targets |
|
| In Vitro | ||||
| In vitro |
INCB054329 shows no significant inhibitory activity against 16 non-BET bromodomains at 3 μM. In a panel of 32 hematologic cancer cell lines derived from acute myeloid leukemia, non-Hodgkin lymphoma, and multiple myeloma, the median 50% growth inhibition (GI50) value of INCB054329 is 152 nM (range, 26-5000 nM). In contrast to tumor cell lines, the GI50 value against T cells isolated from non-diseased donors stimulated ex vivo with IL-2 is 2.435 μM. Growth inhibition correlates with a concentration-dependent accumulation of cells in the G1 phase of the cell cycle. INCB054828 is also a selective kinase inhibitor of the FGFR 1, 2, and 3[1]. In myeloma cell lines, treatment with INCB054329 inhibits expression of c-MYC and induced HEXIM1. In both AML and lymphoma cell lines, INCB054329 induces apoptosis consistent with increased expression of pro-apoptotic regulators[2]. |
|||
|---|---|---|---|---|
| 細胞実験 | 細胞株 | Myeloma, AML, DLBCL cells | ||
| 濃度 | -- | |||
| 反応時間 | 72 h | |||
| 実験の流れ | Cell viability assay |
|||
| In Vivo | ||
| In Vivo |
INCB054329 exhibits high clearance in mice resulting in a short half-life. At exposures that effectively suppressed c-MYC, INCB054329 is found to be efficacious and well tolerated in both the KMS-12-BM and MM1.S xenograft models[1]. In vivo, oral administration of INCB054329 inhibits tumor growth in several models of hematologic cancers[2]. |
|
|---|---|---|
| 動物実験 | 動物モデル | KMS-12-BM tumors established in female Nu/Nu mice |
| 投与量 | 3, 10, 30, or 100 mg/kg | |
| 投与経路 | oral | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02431260 | Terminated | Solid Tumors and Hematologic Malignancy |
Incyte Corporation |
April 14 2015 | Phase 1|Phase 2 |
化学情報
| 分子量 | 348.36 | 化学式 | C19H16N4O3 |
| CAS No. | 1628607-64-6 | SDF | -- |
| Smiles | CC1=C(C(=NO1)C)C2=C3C4=C(C=C2)NC(=O)N4C(CO3)C5=CC=CC=N5 | ||
| 保管 | 3 years -20°C powder | ||
|
In vitro |
DMSO : 70 mg/mL ( (200.94 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Ethanol : 70 mg/mL Water : ˂1 mg/mL |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
| Clear solution |
5%DMSO
40%
5%
50%ddH2O
|
3.5mg/ml (10.05mM) | Taking the 1 mL working solution as an example, add 50 μL of 70 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
95% Corn oil
|
0.43mg/ml (1.23mM) | Taking the 1 mL working solution as an example, add 50 μL of 8.6 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. | ||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
技術サポート
ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。
他に質問がある場合は、お気軽にお問い合わせください。
* 必須
Tags: INCB054329を買う | INCB054329 ic50 | INCB054329供給者 | INCB054329を購入する | INCB054329費用 | INCB054329生産者 | オーダーINCB054329 | INCB054329化学構造 | INCB054329分子量 | INCB054329代理店
納期
国内在庫品：受注日の翌日（15時までの受注分）
＊北海道、九州、沖縄への配送は受注日より２日以上
を要する場合あり
海外在庫品：受注後１〜２週間