product name Ro3280
Description: RO3280, also known as Ro5203280, is a potent and highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM. RO3280 showed strong antitumor activity in xenograft mouse models. 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.
References: Bioorg Med Chem Lett. 2012 Jan 15;22(2):1247-50.
543.61
Formula
C27H35F2N7O3
CAS No.
1062243-51-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (184.0 mM)
Water: <1 mg/mL
Ethanol: 100 mg/mL (184.0 mM)
Solubility (In vivo)
Synonyms
Ro5203280
other peoduct :
| In Vitro |
In vitro activity: RO3280 shows the strong anti-proliferative activity against lung cancer cell line H82, colorectal cancer cell HT-29, breast cancer cell MDA-MB-468, prostate cancer cell PC3 and skin cancer cell A375 with IC50s of 5, 10, 19, 12 and 70 nM, respectively. Kinase Assay: Cell Assay: When tested with a panel of acute leukemia cell lines, Ro3280 showed inhibitory function on U937, HL 60, NB4, K562, MV4-11, and CCRF with IC50 value of 186 nM, 175 nM, 74 nM, 797 nM, 120 nM, and 162 nM, respectively. It was interesting to notice that ALL cells (35.49-110.76 nM) were more sensitive to Ro3280 compared with AML cells (IC50, 52.80-147.50 nM). Further, it was showed that Ro3280 treatment decreased cell viability, induced apoptosis and disrupted cell cycle [3]. In H82 (lung cancer), HT-29 (colon cancer), MDA-MB-468 (breast cancer), PC3 (prostate cancer), and A375 (cutaneum carcinoma), Ro3280 treatment inhibited PLK1 with the IC50 was 5 nM, 10 nM, 19 nM, 12 nM, and 70 nM, respectively. |
|---|---|
| In Vivo | Nude mice bearing HT-29 xenografts administered with MLN0905 (6.25 mg/Kg – 50 mg/Kg, p.o.) shows dose-dependent pharmacodynamic responses (48 hours after treatment). OCI LY-19-Luc tumor bearing mice administered with MLN0905 (3.12 mg/Kg – 6.25 mg/Kg, p.o.) shows significant pharmacodynamic responses amd peaks at 8 hours after treatment. MLN0905 shows antitumor efficacy in treatment with OCI LY-19-Luc xenografts bearing scid mice for 21 days. The T/C of 6.25 mg/Kg daily group is 0.15. |
| Animal model | RO3280 displays robust antitumor activity in nude mouse implanted with HT-29 human colorectal tumors ranging from 72% tumor growth inhibition when dosed once weekly at 40 mg/kg, to complete tumor regression when dosed more frequently |
| Formulation & Dosage | |
| References | Bioorg Med Chem Lett. 2012 Jan 15;22(2):1247-50. |
