CFI-400437 | CAS# 1169211-37-3 | PLK4 Inhibitor

MedKoo Cat#: 564987 | Name: CFI-400437

Description:

WARNING: This product is for research use only, not for human or veterinary use.

CFI-400437 is a potent and selective inhibitor of polo-like kinase 4 (PLK4). The family of Polo-like kinases is important in the regulation of mitotic progression; this work keys on one member, namely Polo-like kinase 4 (PLK4). PLK4 has been identified as a candidate anticancer target which prompted a search for potent and selective inhibitors of PLK4.

Chemical Structure

CFI-400437

CAS#1169211-37-3 (free base)

Theoretical Analysis

MedKoo Cat#: 564987

Name: CFI-400437

CAS#: 1169211-37-3 (free base)

Chemical Formula: C29H28N6O2

Exact Mass: 492.2274

Molecular Weight: 492.58

Elemental Analysis: C, 70.71; H, 5.73; N, 17.06; O, 6.50

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

1169211-37-3 (free base) 1247000-76-5 (HCl)

Synonym

CFI400437; CFI 400437; CFI-400437

IUPAC/Chemical Name

5-Methoxy-3-(3-{2-[6-(4-methyl-piperazin-1-yl)-pyridin-3-yl]-vinyl}-1H-indazol-6-ylmethylene)-1,3-dihydro-indol-2-one

InChi Key

GBUDRABUNBYJKG-NPNRQVEVSA-N

InChi Code

InChI=1S/C29H28N6O2/c1-34-11-13-35(14-12-34)28-10-5-19(18-30-28)4-8-26-22-7-3-20(16-27(22)33-32-26)15-24-23-17-21(37-2)6-9-25(23)31-29(24)36/h3-10,15-18H,11-14H2,1-2H3,(H,31,36)(H,32,33)/b8-4+,24-15-

SMILES Code

O=C1NC2=C(C=C(OC)C=C2)/C1=C/C3=CC4=C(C=C3)C(/C=C/C5=CC=C(N6CCN(C)CC6)N=C5)=NN4

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Polo-like kinase 4 (PLK4) is a cell cycle-regulated protein kinase (PK) recruited at the centrosome in dividing cells. Its overexpression triggers centrosome amplification, which is associated with genetic instability and carcinogenesis.

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 492.58 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Suri A, Bailey AW, Tavares MT, Gunosewoyo H, Dyer CP, Grupenmacher AT, Piper DR, Horton RA, Tomita T, Kozikowski AP, Roy SM, Sredni ST. Evaluation of Protein Kinase Inhibitors with PLK4 Cross-Over Potential in a Pre-Clinical Model of Cancer. Int J Mol Sci. 2019 Apr 29;20(9):2112. doi: 10.3390/ijms20092112. PMID: 31035676; PMCID: PMC6540285. 2: Laufer R, Forrest B, Li SW, Liu Y, Sampson P, Edwards L, Lang Y, Awrey DE, Mao G, Plotnikova O, Leung G, Hodgson R, Beletskaya I, Mason JM, Luo X, Wei X, Yao Y, Feher M, Ban F, Kiarash R, Green E, Mak TW, Pan G, Pauls HW. The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. J Med Chem. 2013 Aug 8;56(15):6069-87. doi: 10.1021/jm400380m. Epub 2013 Jul 26. PMID: 23829549.