Centrinone-B


Catalog No. Size PriceQuantity
M18192-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

Centrinone-B (LCR-323) is a potent and highly selective PLK4 inhibitor, with a Ki of 0.59 nM.

Product information

CAS Number: 1798871-31-4

Molecular Weight: 631.67

Formula: C27H27F2N7O5S2

Chemical Name: 2-({2-fluoro-4-[(2-fluoro-3-nitrophenyl)methanesulfonyl]phenyl}sulfanyl)-5-methoxy-N-(5-methyl-1H-pyrazol-3-yl)-6-(piperidin-1-yl)pyrimidin-4-amine

Smiles: CC1=CC(NC2N=C(N=C(C=2OC)N2CCCCC2)SC2C=CC(=CC=2F)S(=O)(=O)CC2=CC=CC(=C2F)[N+]([O-])=O)=NN1

InChiKey: UPZNTUYHCRQOIQ-UHFFFAOYSA-N

InChi: InChI=1S/C27H27F2N7O5S2/c1-16-13-22(34-33-16)30-25-24(41-2)26(35-11-4-3-5-12-35)32-27(31-25)42-21-10-9-18(14-19(21)28)43(39,40)15-17-7-6-8-20(23(17)29)36(37)38/h6-10,13-14H,3-5,11-12,15H2,1-2H3,(H2,30,31,32,33,34)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 25 mg/mL (39.58 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Centrinone-B (LCR-323) is a potent and highly selective PLK4 inhibitor, with a Ki of 0.59 nM. Centrinone-B slightly binds to Aurora A and Aurora B, with Kis of 1239 nM and 5597.14 nM. Centrinone-B (LCR-323) exhibits >1000-fold selectivity for Plk4 over Aurora A/B in vitro and does not affect cellular Aurora A or B substrate phosphorylation at concentrations that deplete centrosomes. Centrinone-B (LCR-323) (0-200 nM) significantly decreases cell viability of PLK4-centriole conjunction melanoma cell lines except p53 mutant SK-MEL-28, and this effect is via inhibition of PLK4. Inhibition of PLK4 by Centrinone-B (LCR-323) also induces apoptosis in human melanoma cell lines.

Products are for research use only. Not for human use.

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