カタログ番号 T73033 CAS
2904690-41-9
TRK II-IN-1 is a potent type II inhibitor of tropomyosin receptor kinases (TRK), demonstrating inhibitory half-maximal inhibitory concentrations (IC50s) of 3.3, 6.4, 4.3, and 9.4 nM against TRKA, TRKB, TRKC, and the mutant TRKA G667C, respectively. Additionally, this compound exhibits IC50 values of 1.3 nM against FLT3, 9.9 nM against RET, and 71.1 nM against VEGFR2. TRK II-IN-1 primarily serves as a research tool for studying TRK-driven cancers [1].
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TRK II-IN-1, CAS 2904690-41-9
| パッケージサイズ |
在庫状況 |
単価(税別) |
| 25 mg |
約6-8 週間 |
￥ 349,000 |
| 50 mg |
約6-8 週間 |
￥ 454,500 |
| 100 mg |
約6-8 週間 |
￥ 574,000 |
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生物学的特性に関する説明
化学的特性
保存条件
& 溶解度情報
| 説明 |
TRK II-IN-1 is a potent type II inhibitor of tropomyosin receptor kinases (TRK), demonstrating inhibitory half-maximal inhibitory concentrations (IC50s) of 3.3, 6.4, 4.3, and 9.4 nM against TRKA, TRKB, TRKC, and the mutant TRKA G667C, respectively. Additionally, this compound exhibits IC50 values of 1.3 nM against FLT3, 9.9 nM against RET, and 71.1 nM against VEGFR2. TRK II-IN-1 primarily serves as a research tool for studying TRK-driven cancers [1]. |
| ターゲット＆IC50 |
TrkA:3.3 nM, TrkB:6.4 nM, TrkC:4.3 nM, FLT3:1.3 nM, RET:9.9 nM, VEGFR2:71.1 nM, TrkA G667C:9.4 nM
|
| In vitro |
TRK II-IN-1 (compound 12d) exhibited potent kinase inhibition activity, with over 90% inhibition of VEGFR2, RET, FLT3, and approximately 70% inhibition of Kit, CSF1R, DDR1, and DDR2 at 1 μM concentration [1]. At 72 hours, the compound effectively inhibited growth in Ba/F3 cell lines Ba/F3-CD74-TRKA, Ba/F3-ETV6-TRKB, and Ba/F3-ETV6-TRKC, with respective IC50 values of 26.1, 44.7, and 15.7 nM [1]. It also hindered proliferation across a range of Ba/F3 cells harboring various types of TRK fusion proteins, including wild type and mutant forms, showing IC50 values between 2.6 and 143.3 nM [1]. Furthermore, TRK II-IN-1 induced apoptosis in Ba/F3-CD74-TRKA and Ba/F3-CD74-TRKA G667C cells within a 48-hour exposure at concentrations spanning 0.4-500 nM [1], caused G0/G1 cell cycle arrest in the same cells over 24 hours [1], and dose-dependently suppressed phosphorylation of TRKA, TRKA G667C, AKT, ERK, and PLCγ1 after 6 hours of treatment within the range of 0.8-500 nM [1].
|
| 分子量 |
564.6
|
| 分子式 |
C29H31F3N8O |
| CAS No. |
2904690-41-9 |
保存条件
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
投与量変換
You can also refer to dose conversion for different animals.
詳細
In vivo投与量計算 (透明溶液)
ステップ1: 以下の情報を入力してください
溶媒の組成を入力してください
計算器
モル濃度計算機
希釈計算機
再構成計算
分子量計算機
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技術サポート
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Keywords
TRK II-IN-1
2904690-41-9
Tyrosine Kinase/Adaptors
Trk receptor
Inhibitor
inhibitor
inhibit
