AZ82 |
| رقم الكتالوجGC18956 |
AZ82 هو مثبط انتقائي يشبه بروتين KIFC1 (HSET / KIFC1) يشبه كينيسين ، مع Ki من 43 نانومتر و IC50 من 300 نانومتر لـ KIFC1
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Cas No.: 1449578-65-7
Sample solution is provided at 25 µL, 10mM.
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AZ82 is a small molecule inhibitor of KIFC1/HSET, a kinesin-14 family protein that is important for assembling bipolar spindles in cancer cells containing supernumerary centrosomes.[1] AZ82 binds to the KIFC1/microtubule complex and inhibits its microtubule-stimulated activity (IC50 = 300 nM) in an ATP-competitive (Ki = 43 nM) and microtubule-noncompetitive manner but does not inhibit basal KIFC1 activity at a concentration of 100 uM. [2] It is selective for KIFC1 over a panel of nine kinesin motor proteins at a concentration of 5 uM. AZ82 induces multipolar spindle formation in cancer cell lines with high (BT549), but not low (HeLa and MCF-7), numbers of extra chromosomes.
Reference:
[1]. Godinho, S.A., and Pellman, D. Causes and consequences of centrosome abnormalities in cancer. Philos. Trans. R. Soc. Lond. B Biol. Sci. 369(1650), pii: 20130467 (2014).
[2]. Wu, J., Mikule, K., Wang, W., et al. Discovery and mechanistic study of a small molecule inhibitor for motor protein KIFC1. ACS Chem. Biol. 8(10), 2201-2208 (2013).
| Cas No. | 1449578-65-7 | SDF | |
| Chemical Name | αR-[[(5-methyl-4-propyl-2-thienyl)carbonyl]amino]-N-(3R)-3-pyrrolidinyl-6-[3-(trifluoromethoxy)phenyl]-3-pyridinepropanamide | ||
| Canonical SMILES | O=C(N[C@@H]1CCNC1)[C@H](NC(C2=CC(CCC)=C(C)S2)=O)CC3=CC=C(C4=CC(OC(F)(F)F)=CC=C4)N=C3 | ||
| Formula | C28H31F3N4O3S | M.Wt | 560.6 |
| الذوبان | DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 20 mg/ml,Ethanol:PBS (pH 7.2) (1:3): 0.25 mg/ml | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7838 mL | 8.919 mL | 17.838 mL |
| 5 mM | 0.3568 mL | 1.7838 mL | 3.5676 mL |
| 10 mM | 0.1784 mL | 0.8919 mL | 1.7838 mL |
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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 ddH2O, 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
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)
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