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(1E)-CFI-400437 dihydrochloride

Katalog-Nr.GC62728

(1E)-CFI-400437-Dihydrochlorid ist ein potenter PLK4-Inhibitor (IC50 = 0,6 nM) und selektiv gegenÜber anderen Mitgliedern der PLK-Familie (> 10 μM). (1E)-CFI-400437-Dihydrochlorid hemmt Aurora A, Aurora B, KDR und FLT-3 mit IC50-Werten von 0,37, 0,21, 0,48 bzw. 0,18 μM. Antiproliferative AktivitÄt.

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(1E)-CFI-400437 dihydrochloride Chemische Struktur

Cas No.: 1247000-76-5

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5 mg
189,00 $
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10 mg
288,00 $
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25 mg
585,00 $
Auf Lager
50 mg
891,00 $
Auf Lager
100 mg
1.305,00 $
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

(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.

Chemical Properties

Cas No. 1247000-76-5 SDF
Formula C29H30Cl2N6O2 M.Wt 565.49
Löslichkeit 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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
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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Berechnen

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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.

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