1. Cell Cycle/DNA Damage
  2. Polo-like Kinase (PLK)

Ro3280 

Cat. No.: HY-15161 Purity: 99.85%
Handling Instructions

Ro3280 is a potent, highly selective inhibitor of PLK1 with an IC50 and a Kd of 3 nM and 0.09 nM, respectively, and nearly has no effect on PLK2 and PLK3.

For research use only. We do not sell to patients.

Ro3280 Chemical Structure

Ro3280 Chemical Structure

CAS No. : 1062243-51-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 215 In-stock
Estimated Time of Arrival: December 31
2 mg USD 120 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 228 In-stock
Estimated Time of Arrival: December 31
50 mg USD 900 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

View All Polo-like Kinase (PLK) Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Ro3280 is a potent, highly selective inhibitor of PLK1 with an IC50 and a Kd of 3 nM and 0.09 nM, respectively, and nearly has no effect on PLK2 and PLK3.

IC50 & Target[2]

PLK1

0.09 nM (Kd)

ALK

230 nM (Kd)

CAMKK1

1100 nM (Kd)

CAMKK2

87 nM (Kd)

DAPK1

100 nM (Kd)

DAPK3

70 nM (Kd)

FER

53 nM (Kd)

GAK

87 nM (Kd)

MYLK

170 nM (Kd)

PTK2

84 nM (Kd)

PTK2B

130 nM (Kd)

RPS6KA6 (KinDom.2)

560 nM (Kd)

TTK

51 nM (Kd)

In Vitro

Ro3280 (RO3280) inhibits PLK1 activity in NB4 and K562 cells, with an IC50s of 13.45 nM and 301 nM, respectively. RO3280 shows inhibitory activities against the growth of six leukemia cells, with IC50s of 186 nM, 175 nM, 74 nM, 797 nM, 120 nM and 162 nM for U937, HL60, NB4, K562, MV4-11 and CCRF cell lines, respectively. RO3280 also suppresses the growth of primary ALL and AML cells, with IC50s of 35.49-110.76 nM, and 52.80-147.50 nM, respectively. RO3280 (50 or 100 nM) induces apoptosis and cell cycle disorder in acute leukemia cells[1]. Ro3280 shows potent activity in H82, H69, A549 lung cancer cell lines with EC50s of 6 nM, 7 nM and 82 nM. Ro3280 also inhibits several other cancer cell lines, with low concentration[2]. RO3280 is cytotoxic to 5637 and T24 human bladder cancer cells, with IC50s of appr 100 nM.

In Vivo

Ro3280 (RO3280, 40 mg/kg, i.v.) inhibits 72% tumor growth in a mouse xenograft model implanted with HT-29 colorectal cancer cells, and when dosed more frequently, RO3280 completely suppresses the tumor growth[2]. RO3280 (30 mg/kg, once every 5 days, i.p.) shows significant anti-bladder cancer activities in a nude mouse model[3].

Solvent & Solubility
In Vitro: 

DMSO : 6.4 mg/mL (11.77 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8396 mL 9.1978 mL 18.3955 mL
5 mM 0.3679 mL 1.8396 mL 3.6791 mL
10 mM 0.1840 mL 0.9198 mL 1.8396 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

Leukemia cells or primary leukemia cells (2 × 104) are seeded in 96-well plates overnight and incubated with DMSO, or increasing concentrations of RO3280 (0.05-120 μM) for 24 h. The same volume of DMSO added to the vehicle treated wells. Each drug concentration is replicated four times. Then, 10 μL CCK8 solution is added to each well, incubated at 37°C for 2-4 h and the optical density (OD) values are measured at 450 nm using a scanning multi-well spectrophotometer. Relative survival rate is calculated from the absorbance values compared with the control group. The proliferation of cells is calculated as a percentage of the DMSO-treated control wells with 50% inhibitory concentration (IC50) values derived after plotting proliferation values on a logarithmic curve. The IC50 of PLK1 inhibitor is calculated by Graph Prism software[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Briefly, mice (female, 4-5 weeks of age) are used in the assay. Cells (5 × 106 cells in 150 μL) are suspended in RPMI 1640 and injected subcutaneously into the flank of each BALB/c nude mouse. On day 5, tumour size is measured, the animals are randomized into two groups (n = 15 per group), and RO3280 (40 mg/kg, once every 5 days) treatment is initiated by intraperitoneal injection. The control group is treated with vehicle (1.5% DMSO in PBS). The drug (or vehicle) treatment is performed for 40 days. The length and width of the resulting tumours (in millimetres) are measured every 3 days with callipers. The tumour diameter is measured, and the volume (length × width2 × 0.52) is calculated. The mice are humanely killed on day 45, and the tumours are dissected and weighed. Western blot and immunohistochemistry assays are also performed with these sections. Then, the tumours are fixed, embedded and cut into 3‐μm‐thick sections, which are subsequently stained with haematoxylin and eosin to permit the observation of the tumour margin[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

543.61

Formula

C₂₇H₃₅F₂N₇O₃

CAS No.

1062243-51-9

SMILES

COC1=C(NC2=NC(N(C3CCCC3)CC(F)(F)C(N4C)=O)=C4C=N2)C=CC(C(NC5CCN(C)CC5)=O)=C1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Ro3280
Cat. No.:
HY-15161
Quantity:

Ro3280

Cat. No.: HY-15161