(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.
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- Pureté : 99.51%
- CAS No.: 1655527-68-6
- Formule: C20H27ClN6O
- Masse moléculaire:402.92
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
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 |
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| 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 |
In Vitro
(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.
Chemical Information
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CAS No. 1655527-68-6
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Appearance Solid
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Masse moléculaire 402.92
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2659 KB)
Références
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 |
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| 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 Related Classifications
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