(R)-9b
Based on 1 Customer Validation
(R)-9b is an ATP-competitive kinase inhibitor. (R)-9b binds to the ATP-binding site of ACK1/TNK2, inhibiting their kinase activity and autophosphorylation, with a human IC50 of 56 nM. (R)-9b also inhibits JAK2, Tyk2, ALK, c-Src, ABL1, CHK1, FGFR1, LCK, and ROS/ROS1. (R)-9b can be used for research on prostate cancer.
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。
- 純度 : 99.51%
- CAS 番号: 1655527-68-6
- 分子式: C20H27ClN6O
- 分子量:402.92
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
JAK2 |
Tyk2 |
Abl1 |
TNK2 |
ACK1 |
ALK |
C-src |
Chk1 |
ROS/ROS1 |
FGFR1 |
Lck |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | IC50 |
1.8 μM
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Inhibition of cell growth in human LNCaP prostate cancer cells incubated for 72 hrs by trypan blue exclusion assay.
Inhibition of cell growth in human LNCaP prostate cancer cells incubated for 72 hrs by trypan blue exclusion assay.
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25699576 |
| VCaP | IC50 |
2 μM
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Inhibition of cell growth in human VCaP prostate cancer cells incubated for 72 hrs by trypan blue exclusion assay.
Inhibition of cell growth in human VCaP prostate cancer cells incubated for 72 hrs by trypan blue exclusion assay.
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25699576 |
体外実験
(R)-9b is a potent ACK1 inhibitor with an IC50 of 56 nM in the 33P HotSpot assay[1].
(R)-9b (1 μM) is a potent ACK1 inhibitor with IC50 values in the low nanomolar range for JAK2 (6 nM) and Tyk2 (5 nM), and exhibits good selectivity over other kinases such as ALK (143 nM) and cSrc (438 nM)[1].
(R)-9b (5 μM; 16 h) potently inhibits EGF-induced ACK1 autophosphorylation at Tyr284 in LAPC4 prostate cancer cells, achieving 93.5% inhibition at 5 μM[1].
(R)-9b (2-10 μM; 72 h) effectively suppresses proliferation of LNCaP (IC50 = 1.8 μM) and VCaP (IC50 = 2 μM) prostate cancer cell lines, and shows comparable growth suppression to reference compounds in LAPC4 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LAPC4
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Concentration:5 μM
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Incubation Time:16 h
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Result:Inhibited ACK1 Tyr phosphorylation by 93.5%.
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Cell Line:LNCaP, LAPC4, VCaP
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Concentration:2 μM; 4 μM; 6 μM; 8 μM; 10 μM
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Incubation Time:72 h
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Result:Inhibited cell growth with an IC50 of 1.8 μM in LNCaP cells.
Suppressed cell proliferation comparably to AIM-100 and (S)-9b in LAPC4 cells.
Inhibited cell growth with an IC50 of 2 μM in VCaP cells.
化学情報
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CAS 番号 1655527-68-6
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性状 Solid
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分子量 402.92
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分子式 C20H27ClN6O
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Color White to off-white
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SMILES
CN1CCN(C2=CC=C(NC3=NC=C(Cl)C(NC[C@@H]4OCCC4)=N3)C=C2)CC1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 25 mg/mL (62.05 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4819 mL | 12.4094 mL | 24.8188 mL | 62.0471 mL |
| 5 mM | 0.4964 mL | 2.4819 mL | 4.9638 mL | 12.4094 mL | |
| 10 mM | 0.2482 mL | 1.2409 mL | 2.4819 mL | 6.2047 mL | |
| 15 mM | 0.1655 mL | 0.8273 mL | 1.6546 mL | 4.1365 mL | |
| 20 mM | 0.1241 mL | 0.6205 mL | 1.2409 mL | 3.1024 mL | |
| 25 mM | 0.0993 mL | 0.4964 mL | 0.9928 mL | 2.4819 mL | |
| 30 mM | 0.0827 mL | 0.4136 mL | 0.8273 mL | 2.0682 mL | |
| 40 mM | 0.0620 mL | 0.3102 mL | 0.6205 mL | 1.5512 mL | |
| 50 mM | 0.0496 mL | 0.2482 mL | 0.4964 mL | 1.2409 mL | |
| 60 mM | 0.0414 mL | 0.2068 mL | 0.4136 mL | 1.0341 mL |
(R)-9b 関連分類
HY-113787 関連分類
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