CFI-400437
- Product Name
- CFI-400437
- CAS No.
- 1247000-76-5
- Chemical Name
- CFI-400437
- Synonyms
- CS-2656;CFI-400437;CFI-400437 HCl;CFI 400437;CFI400437;(1E)-CFI-400437 2HCl;CFI-400437 dihydrochloride;(1E)-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
- CBNumber
- CB13167321
- Molecular Formula
- C29H29ClN6O2
- Formula Weight
- 529.04
- MOL File
- 1247000-76-5.mol
CFI-400437 Property
- 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 and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P330Rinse mouth.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- SYN1207
- Product name
- CFI-400437
- Packaging
- 5mg
- Price
- $410
- Updated
- 2021/12/16
- Product number
- SYN-1207-M100
- Product name
- CFI-400437
- Purity
- ≥95%
- Packaging
- 100mg
- Price
- $3186
- Updated
- 2021/12/16
- Product number
- DC10069
- Product name
- CFI-400437
- Purity
- >98%
- Packaging
- 10mg
- Price
- $400
- Updated
- 2021/12/16
- Product number
- DC10069
- Product name
- CFI-400437
- Purity
- >98%
- Packaging
- 50mg
- Price
- $1100
- Updated
- 2021/12/16
- Product number
- DC10069
- Product name
- CFI-400437
- Purity
- >98%
- Packaging
- 100mg
- Price
- $1900
- Updated
- 2021/12/16
CFI-400437 Chemical Properties,Usage,Production
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. |
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
Raw materials
Preparation Products
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