ChemicalBook Product Catalog Biochemical Engineering Inhibitors Cell Cycle CDK inhibitors Ro 3306

Ro 3306

Product NameRo 3306
CAS872573-93-8
MFC18H13N3OS2
MW351.45
EINECS
MOL File872573-93-8.mol

Chemical Properties

Boiling point	569.1±60.0 °C(Predicted)
Density	1.41
storage temp.	2-8°C
solubility	DMSO: soluble5mg/mL, clear
pka	3.99±0.10(Predicted)
form	powder
color	white to light brown
Stability	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
InChI	1S/C18H13N3OS2/c22-17-16(24-18(21-17)20-11-14-4-2-8-23-14)10-12-5-6-15-13(9-12)3-1-7-19-15/h1-10H,11H2,(H,20,21,22)/b16-10-
InChIKey	XOLMRFUGOINFDQ-YBEGLDIGSA-N
SMILES	O=C1N=C(NCC2=CC=CS2)S/C1=C\C3=CC4=C(C=C3)N=CC=C4

Safety Information

WGK Germany	3
Storage Class	11 - Combustible Solids

Usage And Synthesis

Description

RO-3306 (872573-93-8) is a selective inhibitor of CDK1 (IC50= 35 nM versus CDK2 IC50= 340nM).1,2It induces G2/M phase cell cycle arrest and apoptosis. Inhibition of CDK1 with RO-3306 has been shown to have synergistic effects with PARP inhibitors in treating various breast cancers.3,4It has also been demonstrated to overcome apoptotic resistance in BRAFV600Ehuman colorectal cancer cells.5

Uses

RO-3306 is an ATP-competitive and selective CDK1 inhibitor used against a diverse panel of human kinases. Used in the treatment of malignant tumors in conjunction with PARP inhibitors.

Uses

RO-3306 has been used:

To study the significance of CA4-mediated cytotoxicity in mitotic arrest
In cell cycle synchronization to conduct a study on proteomics
As a CDK1 inhibitor, to prevent early mitotic entry

Biochem/physiol Actions

RO-3306 is a selective ATP-competitive inhibitor of CDK1. It inhibites CDK1 cyclin B1 activity with Ki of 35 nM, nearly 10-fold selectivity relative to CDK2/cyclin E and over 50-fold relative to CDK4/cyclin D. RO-3306 has been used to cause cell cycle arrest at the G2/M boundary.

IC 50

CDK1: 20 nM (Ki); CDK1/cyclinB1: 35 nM (Ki); CDK1/cyclin A: 110 nM (Ki); CDK2/cyclinE: 340 nM (Ki); PKCδ: 318 nM (Ki); SGK: 497 nM (Ki); ERK: 1980 nM (Ki)

storage

Store at +4°C

References

[1] LYUBOMIR T VASSILEV. Selective small-molecule inhibitor reveals critical mitotic functions of human CDK1.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2006: 10660-10665. DOI:10.1073/pnas.0600447103
[2] LILIANA KRASINSKA Daniel F Emilie Cot. Selective chemical inhibition as a tool to study Cdk1 and Cdk2 functions in the cell cycle.[J]. Cell Cycle, 2008: 1702-1708. DOI:10.4161/cc.7.12.6101
[3] AISLING PIERCE. Comparative antiproliferative effects of iniparib and olaparib on a panel of triple-negative and non-triple-negative breast cancer cell lines.[J]. Cancer Biology & Therapy, 2013, 14 6: 537-545. DOI:10.4161/cbt.24349
[4] QING XIA. The CDK1 inhibitor RO3306 improves the response of BRCA-proﬁcient breast cancer cells to PARP inhibition.[J]. International journal of oncology, 2014, 44 3: 735-744. DOI:10.3892/ijo.2013.2240
[5] PENG ZHANG. Targeting CDK1 and MEK/ERK Overcomes Apoptotic Resistance in BRAF-Mutant Human Colorectal Cancer.[J]. Molecular Cancer Research, 2018, 16 3: 378-389. DOI:10.1158/1541-7786.mcr-17-0404

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