RO-3280 | CAS#1062243-51-9 | PLK1 inhibitor

MedKoo Cat#: 406354 | Name: RO-3280

Description:

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

RO-3280, also known as Ro5203280, is a potent and selective PLK 1 inhibitor with excellent in vitro cellular potency. RO3280 showed strong antitumor activity in xenograft mouse models. he 50% inhibitory concentration (IC50) of RO3280 for acute leukemia cells was between 74 and 797 nM. The IC50 of RO3280 in primary acute lymphocytic leukemia (ALL) and AML cells was between 35.49 and 110.76 nM and 52.80 and 147.50 nM, respectively. RO3280 induced apoptosis and cell cycle disorder in leukemia cells. RO3280 treatment regulated several apoptosis-associated genes. Polo-like kinase 1 (PLK1) is highly expressed in many cancers and therefore a biomarker of transformation and potential target for the development of cancer-specific small molecule drugs.

Chemical Structure

RO-3280

CAS#1062243-51-9

Theoretical Analysis

MedKoo Cat#: 406354

Name: RO-3280

CAS#: 1062243-51-9

Chemical Formula: C27H35F2N7O3

Exact Mass: 543.2769

Molecular Weight: 543.61

Elemental Analysis: C, 59.65; H, 6.49; F, 6.99; N, 18.04; O, 8.83

Price and Availability

Size	Price	Availability
5mg	USD 110.00	Ready to ship
10mg	USD 190.00	Ready to ship
25mg	USD 385.00	Ready to ship
50mg	USD 650.00	Ready to ship
100mg	USD 1,150.00	Ready to ship
200mg	USD 1,950.00	Ready to ship

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

No Data

Synonym

RO3280; RO-3280; RO 3280; Ro5203280; Ro-5203280; Ro 5203280.

IUPAC/Chemical Name

4-((9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino)-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide

InChi Key

DJNZZLZKAXGMMC-UHFFFAOYSA-N

InChi Code

InChI=1S/C27H35F2N7O3/c1-34-12-10-18(11-13-34)31-24(37)17-8-9-20(22(14-17)39-3)32-26-30-15-21-23(33-26)36(19-6-4-5-7-19)16-27(28,29)25(38)35(21)2/h8-9,14-15,18-19H,4-7,10-13,16H2,1-3H3,(H,31,37)(H,30,32,33)

SMILES Code

O=C(NC1CCN(C)CC1)C2=CC=C(NC3=NC=C(N4C)C(N(C5CCCC5)CC(F)(F)C4=O)=N3)C(OC)=C2

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

0 Â– 4 C for short term (weeks to 1 month) or -20 C for long terms (months to years).

Solubility

Soluble in DMSO, DMF, and ethanol

Shelf Life

>2 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

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#A24T05K16

QC Data

View QC data: current batch, Lot#A24T05K16

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

Ro 3280 is a selective PLK1 inhibitor with IC50 values of 3 and 6 nM in an enzymatic assay and H82 lung cancer cells, respectively. Ro 3280 is over 500-fold selective for PlK1 over a panel of 318 kinases. It inhibits tumor growth in a mouse xenograft model using the HT-29 colorectal cancer cell line, increases autophagy and mTOR phosphorylation in NB4 acute myeloid leukemia cells, and induces apoptosis in human bladder cancer and leukemia cells.

In vitro activity:

Ro 3280 induces tumor suppression both in vitro and in vivo. An inhibitory effect was observed with the highly proliferating cancer cell lines tested, but not with the nontumorigenic cell line. Ro 3280 induces G2-M cell-cycle arrest and apoptosis. Western blotting shows it inhibits PLK1 phosphorylation, downregulates Cdc25c, and upregulates Wee1 and Securin as well as the DNA damage-related factor Chk2 in vitro and in vivo. Reference: Mol Cancer Ther. 2013 Aug;12(8):1393-401. https://pubmed.ncbi.nlm.nih.gov/23686835/

In vivo activity:

Electric field stimulation-induced contractions of prostate strips were reduced by Ro 3280 (100 nM). RT-PCR, Western blot, and immunofluorescence suggested expression of PLK1 in the human prostate. PLK-dependent signaling may be a new pathway, which promotes α1-adrenergic contraction of prostate smooth muscle cells. Reference: Front Physiol. 2018 Jun 15;9:734. https://pubmed.ncbi.nlm.nih.gov/29962965/

	Solvent	mg/mL	mM
Solubility
	DMSO	30.0	55.19
	DMF	30.0	55.19
	Ethanol	30.0	55.19

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 543.61 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.

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. Cheung AK, Ip JC, Lung HL, Wu JZ, Tsao SW, Lung ML. Polo-like kinase inhibitor Ro5203280 has potent antitumor activity in nasopharyngeal carcinoma. Mol Cancer Ther. 2013 Aug;12(8):1393-401. doi: 10.1158/1535-7163.MCT-12-1219. Epub 2013 May 17. PMID: 23686835. 2. Hennenberg M, Kuppermann P, Yu Q, Herlemann A, Tamalunas A, Wang Y, Rutz B, Ciotkowska A, Strittmatter F, Stief CG, Gratzke C. Inhibition of Prostate Smooth Muscle Contraction by Inhibitors of Polo-Like Kinases. Front Physiol. 2018 Jun 15;9:734. doi: 10.3389/fphys.2018.00734. PMID: 29962965; PMCID: PMC6013909.

In vitro protocol:

In vivo protocol:

1. Hennenberg M, Kuppermann P, Yu Q, Herlemann A, Tamalunas A, Wang Y, Rutz B, Ciotkowska A, Strittmatter F, Stief CG, Gratzke C. Inhibition of Prostate Smooth Muscle Contraction by Inhibitors of Polo-Like Kinases. Front Physiol. 2018 Jun 15;9:734. doi: 10.3389/fphys.2018.00734. PMID: 29962965; PMCID: PMC6013909.

1: Chen S, Bartkovitz D, Cai J, Chen Y, Chen Z, Chu XJ, Le K, Le NT, Luk KC, Mischke S, Naderi-Oboodi G, Boylan JF, Nevins T, Qing W, Chen Y, Wovkulich PM. Identification of novel, potent and selective inhibitors of Polo-like kinase 1. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1247-50. doi: 10.1016/j.bmcl.2011.11.052. Epub 2011 Dec 1. PubMed PMID: 22172702.