الصفحة الرئيسية>>Signaling Pathways>> Cell Cycle/Checkpoint>> PLK>>(1E)-CFI-400437 dihydrochloride

(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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(1E)-CFI-400437 dihydrochloride التركيب الكيميائي

Cas No.: 1247000-76-5

الحجم السعر المخزون الكميّة
5 mg
189٫00
متوفر
10 mg
288٫00
متوفر
25 mg
585٫00
متوفر
50 mg
891٫00
متوفر
100 mg
1305٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of (1E)-CFI-400437 dihydrochloride

(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 of (1E)-CFI-400437 dihydrochloride

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.
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 of (1E)-CFI-400437 dihydrochloride

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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In vivo Formulation Calculator (Clear solution) of (1E)-CFI-400437 dihydrochloride

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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. )

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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