| Identification | Back Directory | [Name]
CFI-400437 | [CAS]
1247000-76-5 | [Synonyms]
CS-2656
CFI-400437
CFI-400437 HCl
CFI 400437;CFI400437 | [Molecular Formula]
C29H29ClN6O2 | [MDL Number]
MFCD31922709 | [MOL File]
1247000-76-5.mol | [Molecular Weight]
529.04 |
| Chemical Properties | Back Directory | [storage temp. ]
4°C, protect from light | [solubility ]
DMSO : 12.5 mg/mL (22.10 mM; Need ultrasonic) | [form ]
Solid | [color ]
Brown to orange |
| Hazard Information | Back Directory | [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 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]. | 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) | [storage]
4°C, protect from light | [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 |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
Cckinase, Inc.
|
| Tel: |
+1 (732)236-3202 |
| Website: |
www.cckinase.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|