|
|
| | Ro 3306 Basic information |
| Product Name: | Ro 3306 | | Synonyms: | Ro 3306;2-[[(Thiophen-2-yl)methyl]amino]-5-[1-(quinolin-6-yl)meth-(Z)-ylidene]thiazol-4-one;(Z)-5-(quinolin-6-ylmethylene)-2-(thiophen-2-ylmethylamino)thiazol-4(5H)-one;(5Z)-5-Quinolin-6-ylmethylene-2-[(thiophen-2-ylmethyl)-amino]-thiazol-4-one;5-(6-Quinolinylmethylene)-2-[(2-thienylmethyl)amino]-4(5H)-thiazolone;RO3306;RO 3306;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 | | CAS: | 872573-93-8 | | MF: | C18H13N3OS2 | | MW: | 351.45 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 872573-93-8.mol |  |
| | Ro 3306 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. |
| | Ro 3306 Usage And Synthesis |
| 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 | 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. | | 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 |
| | Ro 3306 Preparation Products And Raw materials |
|