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MedKoo Cat#: 406182 | Name: RO-3306
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Description:

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

RO-3306 is a CDK1 inhibitor with potential anticancer activity. Treatment of growing AML cells with RO-3306 induced G2/M-phase cell cycle arrest and apoptosis in a dose- and time-dependent manner. RO-3306 downregulated expression of the antiapoptotic proteins Bcl-2 and survivin and blocked p53-mediated induction of p21 and MDM2. RO-3306 actively enhances downstream p53 signaling to promote apoptosis.

Chemical Structure

RO-3306
RO-3306
CAS#872573-93-8

Theoretical Analysis

MedKoo Cat#: 406182

Name: RO-3306

CAS#: 872573-93-8

Chemical Formula: C18H13N3OS2

Exact Mass: 351.0500

Molecular Weight: 351.44

Elemental Analysis: C, 61.52; H, 3.73; N, 11.96; O, 4.55; S, 18.24

Price and Availability

Size Price Availability Quantity
10mg USD 150.00 Ready to ship
25mg USD 250.00 Ready to ship
50mg USD 400.00 Ready to ship
100mg USD 700.00 Ready to ship
200mg USD 1,250.00 Ready to ship
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Related CAS #
No Data
Synonym
RO3306; RO 3306; RO-3306
IUPAC/Chemical Name
5-(6-Quinolinylmethylene)-2-[(2-thienylmethyl)amino]-4(5H)-thiazolone
InChi Key
XOLMRFUGOINFDQ-MHWRWJLKSA-N
InChi Code
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+
SMILES Code
O=C1N=C(NCC2=CC=CS2)S/C1=C/C3=CC=C4N=CC=CC4=C3
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, not soluble in water.
Shelf Life
>5 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
        
Biological target:
Ro-3306 is an inhibitor of CDK1, with Kis of 20 nM, 35 nM and 340 nM for CDK1, CDK1/cyclin B1 and CDK2/cyclin E, respectively.
In vitro activity:
To analyze the DNA damage and repair processes during RO-3306-induced G2 arrest, this study examined whether irradiated cells undergoing prolonged G2 arrest repaired DSBs or induced damaged DNA to enter M-phase during RO-3306 treatment. Immediate discontinuation of RO-3306 treatment (10 μM) and exchanged treatment (DMSO or 2 μM) after irradiation in HL-60 cells resulted in mitotic entry and DSB levels significantly higher in M-phase cells, compared to in non-irradiated control (Fig. 4A and B). In contrast, persistent 10 μM RO-3306 treatment for 8 h after irradiation dramatically decreased DSB levels in M-phase cells compared to the immediate release of RO-3306 treatment (Fig. 4C and D). This study showed that further DNA-PK inhibition during prolonged G2 arrest delayed DNA repair and inhibited cell proliferation (supplementary Fig. 2). The clonogenic assay demonstrated that persistent treatment with RO-3306 after irradiation resulted in higher fractions of surviving HeLa cells, supporting the resistance of cells to CDK1 inhibition (Fig. 4E). These results show that even higher dose of RO-3306 induced prolonged G2 arrest, allowing irradiated cells to repair DSBs and preventing DNA damage from being carried over into M-phase. Reference: Biochem Biophys Res Commun. 2021 Apr 23;550:56-61. https://www.sciencedirect.com/science/article/pii/S0006291X21003466?via%3Dihub
In vivo activity:
Subcutaneous tumor xenografts developed from HEC-1-B cells in BALB/c nude mice were successfully established individually. Consistent with the in vitro results, the tumor growth of xenograft endometrial cancer grafts was significantly blocked with the treatment of RO3306 (Figure (5A-D). As early as day 4 of the treatment, there was a extremely significant difference in tumor volume between the RO3306 treatment group and the control group (p <0.0001) (Figure 5A). At the end of the study, tumor volumes of endometrial cancer grafts in the RO3306 treatment group and the control group were 392.2 ± 24.34 and 689.8 ± 104.3mm3, respectively, with highly significant differences between the two groups (p <0.01) (Figure 5A). As to body weight, there was no significant difference between the two groups (p >0.05) (Figure 5B). The tumor weight of endometrial cancer grafts harvested at the end of the study in the RO3306 treatment group was significantly lower than that in the control group (p <0.05) (Figure 5C). These data suggested that CDK1 played an important role in the growth and proliferation of endometrial cancer cells in vivo and RO3306 can serve as its targeted inhibitor for the treatment of endometrioid endometrial cancer. Reference: J Cancer. 2021; 12(8): 2206–2215. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7974891/
Solvent mg/mL mM
Solubility
DMSO 16.3 46.27
DMSO:PBS (pH 7.2) (1:2) 0.3 0.71
DMF 20.0 56.91
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 351.44 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.

Recalculate based on batch purity %
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
Formulation protocol:
1. Sunada S, Saito H, Zhang D, Xu Z, Miki Y. CDK1 inhibitor controls G2/M phase transition and reverses DNA damage sensitivity. Biochem Biophys Res Commun. 2021 Apr 23;550:56-61. doi: 10.1016/j.bbrc.2021.02.117. Epub 2021 Mar 5. PMID: 33684621. 2. Kojima K, Shimanuki M, Shikami M, Andreeff M, Nakakuma H. Cyclin-dependent kinase 1 inhibitor RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis in AML. Cancer Sci. 2009 Jun;100(6):1128-36. doi: 10.1111/j.1349-7006.2009.01150.x. Epub 2009 Mar 10. PMID: 19385969; PMCID: PMC2759356. 3. Ying X, Che X, Wang J, Zou G, Yu Q, Zhang X. CDK1 serves as a novel therapeutic target for endometrioid endometrial cancer. J Cancer. 2021 Feb 22;12(8):2206-2215. doi: 10.7150/jca.51139. PMID: 33758599; PMCID: PMC7974891. 4. Czaplinski S, Hugle M, Stiehl V, Fulda S. Polo-like kinase 1 inhibition sensitizes neuroblastoma cells for vinca alkaloid-induced apoptosis. Oncotarget. 2016 Feb 23;7(8):8700-11. doi: 10.18632/oncotarget.3901. PMID: 26046302; PMCID: PMC4890998.
In vitro protocol:
1. Sunada S, Saito H, Zhang D, Xu Z, Miki Y. CDK1 inhibitor controls G2/M phase transition and reverses DNA damage sensitivity. Biochem Biophys Res Commun. 2021 Apr 23;550:56-61. doi: 10.1016/j.bbrc.2021.02.117. Epub 2021 Mar 5. PMID: 33684621. 2. Kojima K, Shimanuki M, Shikami M, Andreeff M, Nakakuma H. Cyclin-dependent kinase 1 inhibitor RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis in AML. Cancer Sci. 2009 Jun;100(6):1128-36. doi: 10.1111/j.1349-7006.2009.01150.x. Epub 2009 Mar 10. PMID: 19385969; PMCID: PMC2759356.
In vivo protocol:
1. Ying X, Che X, Wang J, Zou G, Yu Q, Zhang X. CDK1 serves as a novel therapeutic target for endometrioid endometrial cancer. J Cancer. 2021 Feb 22;12(8):2206-2215. doi: 10.7150/jca.51139. PMID: 33758599; PMCID: PMC7974891. 2. Czaplinski S, Hugle M, Stiehl V, Fulda S. Polo-like kinase 1 inhibition sensitizes neuroblastoma cells for vinca alkaloid-induced apoptosis. Oncotarget. 2016 Feb 23;7(8):8700-11. doi: 10.18632/oncotarget.3901. PMID: 26046302; PMCID: PMC4890998.
1: Van Matre S, Huq S, Akana L, Eldridge DE, Zuniga O, Rodrigues H, Wolfe AR. Enhanced radiosensitivity of pancreatic cancer achieved through inhibition of Cyclin-dependent kinase 1. Radiother Oncol. 2024 Sep 11;200:110531. doi: 10.1016/j.radonc.2024.110531. Epub ahead of print. PMID: 39270987. 2: Wang J, Guo J, Yu S, Yu H, Kuraz AB, Jilo DD, Cheng G, Li A, Jia C, Zan L. Knockdown of NFIC Promotes Bovine Myoblast Proliferation through the CENPF/CDK1 Axis. J Agric Food Chem. 2024 Jun 5;72(22):12641-12654. doi: 10.1021/acs.jafc.4c01811. Epub 2024 May 23. PMID: 38780097. 3: Tao Y, Li L, Yang X, Yin S, Zhang Z, Wang H, Pu R, Wang Z, Zhang Q, Mu H, Wu C, He J, Yang L. Magnetic-driven hydrogel microrobots for promoting osteosarcoma chemo-therapy with synthetic lethality strategy. Front Chem. 2024 Apr 4;12:1386076. doi: 10.3389/fchem.2024.1386076. PMID: 38638876; PMCID: PMC11024356. 4: Tanaka J, Kuwajima H, Yuki R, Nakayama Y. Simvastatin activates the spindle assembly checkpoint and causes abnormal cell division by modifying small GTPases. Cell Signal. 2024 Jul;119:111172. doi: 10.1016/j.cellsig.2024.111172. Epub 2024 Apr 9. PMID: 38604342. 5: Cui X, Dong H, Luo S, Zhuang B, Li Y, Zhong C, Ma Y, Hong L. Long Non-Coding RNA-Cardiac-Inducing RNA 6 Mediates Repair of Infarcted Hearts by Inducing Mesenchymal Stem Cell Differentiation into Cardiogenic Cells through Cyclin- Dependent Kinase 1. Int J Mol Sci. 2024 Mar 19;25(6):3466. doi: 10.3390/ijms25063466. PMID: 38542439; PMCID: PMC10971150. 6: Kang X, Chen H, Zhou Z, Tu S, Cui B, Li Y, Dong S, Zhang Q, Xu Y. Targeting Cyclin-Dependent Kinase 1 Induces Apoptosis and Cell Cycle Arrest of Activated Hepatic Stellate Cells. Adv Biol (Weinh). 2024 Mar;8(3):e2300403. doi: 10.1002/adbi.202300403. Epub 2023 Dec 16. PMID: 38103005. 7: Hasegawa N, Hongo M, Okada M, Kuga T, Abe Y, Adachi J, Tomonaga T, Yamaguchi N, Nakayama Y. Phosphotyrosine proteomics in cells synchronized at monopolar cytokinesis reveals EphA2 as functioning in cytokinesis. Exp Cell Res. 2023 Nov 1;432(1):113783. doi: 10.1016/j.yexcr.2023.113783. Epub 2023 Sep 17. PMID: 37726045. 8: Huang Y, Fan Y, Zhao Z, Zhang X, Tucker K, Staley A, Suo H, Sun W, Shen X, Deng B, Pierce SR, West L, Yin Y, Emanuele MJ, Zhou C, Bae-Jump V. Inhibition of CDK1 by RO-3306 Exhibits Anti-Tumorigenic Effects in Ovarian Cancer Cells and a Transgenic Mouse Model of Ovarian Cancer. Int J Mol Sci. 2023 Aug 3;24(15):12375. doi: 10.3390/ijms241512375. PMID: 37569750; PMCID: PMC10418904. 9: Vargas-Cortez T, Guerrero-Molina ED, Axosco-Marin J, Vázquez-Ramos JM, Lara- Núñez A. The glycolytic enzymes glyceraldehyde-3-phosphate dehydrogenase and hexokinase interact with cell cycle proteins in maize. FEBS Lett. 2023 Aug;597(16):2072-2085. doi: 10.1002/1873-3468.14704. Epub 2023 Aug 6. PMID: 37489921. 10: Guo E, Yang J, Li L, Chen J, Liu H. TACC3 is an independent prognostic marker, and knockdown of TACC3 enhances the efficacy of CDK1 inhibitor RO3306 in liver cancer cells. J Biochem Mol Toxicol. 2023 Sep;37(9):e23402. doi: 10.1002/jbt.23402. Epub 2023 Jun 21. PMID: 37341435. 11: Ota R, Watanabe T, Wazawa Y, Kuwajima H, Honda T, Soeda S, Saito Y, Yuki R, Fukumoto Y, Yamaguchi N, Yamaguchi N, Nakayama Y. v-Src delocalizes Aurora B by suppressing Aurora B kinase activity during monopolar cytokinesis. Cell Signal. 2023 Sep;109:110764. doi: 10.1016/j.cellsig.2023.110764. Epub 2023 Jun 12. PMID: 37315749. 12: Zheng P, Pan HH, Zhou XH, Qiu YY, Hu J, Qin ZS, Wang TH. Glucose 6 phosphatase dehydrogenase (G6PD): a novel diagnosis marker related to gastrointestinal cancers. Am J Transl Res. 2023 Apr 15;15(4):2304-2328. PMID: 37193179; PMCID: PMC10182507. 13: Chen J, Li M, Liu Y, Guan T, Yang X, Wen Y, Zhu Y, Xiao Z, Shen X, Zhang H, Tang H, Liu T. PIN1 and CDK1 cooperatively govern pVHL stability and suppressive functions. Cell Death Differ. 2023 Apr;30(4):1082-1095. doi: 10.1038/s41418-023-01128-x. Epub 2023 Feb 23. PMID: 36813923; PMCID: PMC10070344. 14: Li D, Wu X, Fan X, Cheng C, Li D, Zhang W. Comprehensive analysis of cuproptosis-related lncRNAs in the prognosis and therapy response of patients with bladder cancer. Ann Transl Med. 2022 Nov;10(22):1232. doi: 10.21037/atm-22-5294. PMID: 36544685; PMCID: PMC9761144. 15: Zhang L, Jiang B, Lan Z, Yang C, Yao Y, Lin J, Wei Q. Immune infiltration landscape on prognosis and therapeutic response and relevant epigenetic and transcriptomic mechanisms in lung adenocarcinoma. Front Immunol. 2022 Oct 6;13:983570. doi: 10.3389/fimmu.2022.983570. PMID: 36275753; PMCID: PMC9582346. 16: Chiu LLY, Subedar OD, Waldman SD. Cell Cycle Synchronization of Primary and Cultured Articular Chondrocytes. Methods Mol Biol. 2022;2579:111-123. doi: 10.1007/978-1-0716-2736-5_9. PMID: 36045202. 17: Heo J, Lee J, Nam YJ, Kim Y, Yun H, Lee S, Ju H, Ryu CM, Jeong SM, Lee J, Lim J, Cho YM, Jeong EM, Hong B, Son J, Shin DM. The CDK1/TFCP2L1/ID2 cascade offers a novel combination therapy strategy in a preclinical model of bladder cancer. Exp Mol Med. 2022 Jun;54(6):801-811. doi: 10.1038/s12276-022-00786-0. Epub 2022 Jun 21. PMID: 35729325; PMCID: PMC9256744. 18: Teo T, Kasirzadeh S, Albrecht H, Sykes MJ, Yang Y, Wang S. An overview of CDK3 in cancer: clinical significance and pharmacological implications. Pharmacol Res. 2022 Jun;180:106249. doi: 10.1016/j.phrs.2022.106249. Epub 2022 May 6. PMID: 35533805. 19: Zhao L, Yan Y, Dai Q, Wang Z, Yin J, Xu Y, Wang Z, Guo X, Li W, Cao R, Zhong W. The CDK1 inhibitor, Ro-3306, is a potential antiviral candidate against influenza virus infection. Antiviral Res. 2022 May;201:105296. doi: 10.1016/j.antiviral.2022.105296. Epub 2022 Mar 30. PMID: 35367281. 20: Wang Z, Chen D, Guan D, Liang X, Xue J, Zhao H, Song G, Lou J, He Y, Zhang H. Material properties of phase-separated TFEB condensates regulate the autophagy-lysosome pathway. J Cell Biol. 2022 May 2;221(5):e202112024. doi: 10.1083/jcb.202112024. Epub 2022 Mar 16. PMID: 35293953; PMCID: PMC8931539.

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