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| | CFI-400437 Basic information |
| Product Name: | CFI-400437 | | Synonyms: | CFI-400437;CFI 400437;CFI400437;CS-2656;CFI-400437 HCl;(1E)-CFI-400437 dihydrochloride;CFI-400437 dihydrochloride;5-Methoxy-3-((3-((E)-2-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)vinyl)-1H-indazol-6-yl)methylene)indolin-2-one dihydrochloride;antiproliferative,Inhibitor,Polo-like Kinase (PLK),anticancer,cells,MCF-7,(1E) CFI 400437 dihydrochloride,PLK4,inhibit,(1E)CFI400437 dihydrochloride | | CAS: | 1247000-76-5 | | MF: | C29H29ClN6O2 | | MW: | 529.04 | | EINECS: | | | Product Categories: | | | Mol File: | 1247000-76-5.mol |  |
| | CFI-400437 Chemical Properties |
| storage temp. | 4°C, protect from light | | solubility | DMSO : 12.5 mg/mL (22.10 mM; Need ultrasonic) | | form | Solid | | color | Brown to orange |
| | CFI-400437 Usage And Synthesis |
| Uses | (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]. | | in vivo | (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 ngh/mL, respectively. The mouse plasma protein binding measurement for (1E)-CFI-400437 is 99%, i.e., unbound compound in plasma is 1%[1]. | Animal Model: | 6-8 week old female CB-17 SCID mice (MDA-MB-468 mouse xenograft model)[1] | | Dosage: | 25 mg/kg | | Administration: | Intraperitoneal injection; daily for 21 days | | Result: | Effective in a mouse xenograft model of tumor growth.
In this study, (1E)-CFI-400437 is weighed and suspended in PEG400:water (30:70) and sonicated at rt for 30 min. The compound is dispensed in aliquots and stored at 20 C° for the duration of the study, and each aliquot was thawed at room temperature before each dose.
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| | IC 50 | PLK4: 0.6 nM (IC50) | | References | [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. DOI:10.1021/jm400380m |
| | CFI-400437 Preparation Products And Raw materials |
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