KX1-004 |
Catalog No.GC10523
One-Click Copy Product Info
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KX1-004는 IC50이 40μM인 강력한 비 ATP 경쟁 Src-PTK 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 518058-84-9
Sample solution is provided at 25 µL, 10mM.
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KX1-004 is a non-ATP competitive inhibitor of pp60c-src with IC50 value of 40 μM [1].
KX1-004 is a close analog of the indole-based Src-PTK inhibitors reported previously. It has a 5-fluoro group and showed potent inhibition activity in isolated Src-PTK assay. KX1-004 was found to have protective effect in noise-induced hearing loss. The chinchillas treated with 30 μM KX1-004 were exposed to continuous noise. And the results showed that treated ears exhibited up to 40 dB less threshold shift (TTS) and up to 25 dB less permanent threshold shift (PTS) than control ears. KX1-004 treatment also significantly reduced outer hair cell (OHC) loss than control. Besides that, KX1-004 was proved to reduce the hearing loss and hair cell loss associated with impulse noise exposure markedly [1, 2].
References:
[1] Harris K C, Hu B, Hangauer D, et al. Prevention of noise-induced hearing loss with Src-PTK inhibitors. Hearing research, 2005, 208(1): 14-25.
[2] Milkiewicz K L, Marsilje T H, Woodworth Jr R P, et al. The design, synthesis and activity of non-ATP competitive inhibitors of pp60 c-src tyrosine kinase. Part 2: Hydroxyindole derivatives. Bioorganic & medicinal chemistry letters, 2000, 10(5): 483-486.
| Cas No. | 518058-84-9 | SDF | |
| Chemical Name | 5-fluoro-N-(3-hydroxybenzyl)-1H-indole-2-carboxamide | ||
| Canonical SMILES | FC1=CC(C=C(C(NCC2=CC=CC(O)=C2)=O)N3)=C3C=C1 | ||
| Formula | C16H13FN2O2 | M.Wt | 284.29 |
| Solubility | ≥ 10.1mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5175 mL | 17.5877 mL | 35.1753 mL |
| 5 mM | 703.5 μL | 3.5175 mL | 7.0351 mL |
| 10 mM | 351.8 μL | 1.7588 mL | 3.5175 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)