(1E)-CFI-400437 dihydrochloride |
رقم الكتالوجGC62728 |
(1E) -CFI-400437 ثنائي هيدروكلوريد هو مثبط قوي PLK4 (IC50 = 0.6 نانومتر) وانتقائي ضد أعضاء آخرين من عائلة PLK (> 10 ميكرومتر)(1E) -CFI-400437 ثنائي هيدروكلوريد يثبط Aurora A و Aurora B و KDR و FLT-3 مع IC50s 0.37 و 0.21 و 0.48 و 0.18 ميكرومتر على التوالينشاط مضاد للتكاثر
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Cas No.: 1247000-76-5
Sample solution is provided at 25 µL, 10mM.
(1E)-CFI-400437 dihydrochloride is a potent PLK4 (IC50= 0.6 nM) inhibitor and selective against other members of the PLK family (>10 μM). (1E)-CFI-400437 dihydrochloride inhibits Aurora A, Aurora B, KDR and FLT-3 with IC50s of 0.37, 0.21, 0.48, and 0.18 μM, respectively. Antiproliferative activity[1].
(1E)-CFI-400437 (25 mg/kg; intraperitoneal injection; daily for 21 days) dihydrochloride shows effective in a mouse xenograft model of tumor growth[1].The plasma levels of (1E)-CFI-400437 (50 mg/kg; IP; mice) dihydrochloride shows a Cmax of 92 ng/mL and AUC of 190 ng•h/mL, respectively. The mouse plasma protein binding measurement for (1E)-CFI-400437 is 99%, i.e., unbound compound in plasma is 1%[1].
[1]. Laufer R, et al. The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. J Med Chem. 2013;56(15):6069-6087.
Cas No. | 1247000-76-5 | SDF | |
Formula | C29H30Cl2N6O2 | M.Wt | 565.49 |
الذوبان | DMSO : 12.5 mg/mL (22.10 mM; Need ultrasonic) | Storage | 4°C, protect from light |
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 | 1.7684 mL | 8.8419 mL | 17.6838 mL |
5 mM | 0.3537 mL | 1.7684 mL | 3.5368 mL |
10 mM | 0.1768 mL | 0.8842 mL | 1.7684 mL |
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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 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: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5
(Based on Reviews and 27 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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