| Identification | Back Directory | [Name]
Ro 3306 | [CAS]
872573-93-8 | [Synonyms]
CS-770
Ro 3306
RO3306;RO 3306
Ro 3306 USP/EP/BP
5-(6-Quinolinylmethylene)-2-[(2-thienylmethyl)amino]-4(5H)-thiazolone
(5Z)-5-Quinolin-6-ylmethylene-2-[(thiophen-2-ylmethyl)-amino]-thiazol-4-one
(Z)-5-(quinolin-6-ylmethylene)-2-(thiophen-2-ylmethylamino)thiazol-4(5H)-one
4(5H)-Thiazolone, 5-(6-quinolinylmethylene)-2-[(2-thienylmethyl)amino]-, (5Z)-
(5Z)-5-(quinolin-6-ylmethylidene)-2-(thiophen-2-ylmethylamino)-1,3-thiazol-4-one
2-[[(Thiophen-2-yl)methyl]amino]-5-[1-(quinolin-6-yl)meth-(Z)-ylidene]thiazol-4-one | [Molecular Formula]
C18H13N3OS2 | [MDL Number]
MFCD17392573 | [MOL File]
872573-93-8.mol | [Molecular Weight]
351.445 |
| Chemical Properties | Back Directory | [Boiling point ]
569.1±60.0 °C(Predicted) | [density ]
1.41 | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble5mg/mL, clear | [form ]
powder | [pka]
3.99±0.10(Predicted) | [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 |
| Hazard Information | Back Directory | [Description]
RO-3306 (872573-93-8) is a selective inhibitor of CDK1 (IC50?= 35 nM versus CDK2 IC50?= 340nM).1,2?It 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.3,4?It has also been demonstrated to overcome apoptotic resistance in BRAFV600E?human colorectal cancer cells.5 | [Uses]
Inhibitor of CDK1/cyclin B1 and CDK1/cyclin A. Reversibly arrests human cells at the G2/M border of the cell cycle. Allows for effective cell synchronisation in early mitosis. Downregulates expression of the antiapoptotic proteins Bcl-2 and survivin and blocks p53-mediated induction of p21 and MDM2. | [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) Vassilev?et al.?(2006),?Selective small-molecule inhibitor reveals critical mitotic functions of human CDK1; Proc. Nat. Acad. Sci. USA?103?10660
2) Krasinska?et al.?(2008),?Selective chemical inhibition as a tool to study Cdk1 and Cdk2 functions in the cell cycle; Cell Cycle?7?1702
3) Pierce?et al.?(2013),?Comparative antiproliferative effects of iniparib and olaparib on a panel of triple-negative and non-triple-negative breast cancer cell lines; Cancer Biol. Ther.?14?537
4) Xia?et al.?(2014),?The CDK1 inhibitor RO3306 improves the response of BRCA-proficient breast cancer cells to PARP inhibition;?Int. J. Oncol.?44?735
5) Zhang?et al.?(2018),?Targeting CDK1 and MEK/ERK Overcomes Apoptotic Resistance in BRAF-Mutant Human Colorectal Cancer; Mol. Cancer Res.?16?378 |
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| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
| Company Name: |
Sigma-Aldrich
|
| Telephone: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
|