Description
RO3280, 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.
Product information
CAS Number: 1062243-51-9
Molecular Weight: 543.61
Formula: C27H35F2N7O3
Chemical Name: 4-({9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-5H,6H,7H,8H,9H-pyrimido[4,5-b][1,4]diazepin-2-yl}amino)-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide
Smiles: CN1CCC(CC1)NC(=O)C1C=C(OC)C(=CC=1)NC1=NC2=C(C=N1)N(C)C(=O)C(F)(F)CN2C1CCCC1
InChiKey: DJNZZLZKAXGMMC-UHFFFAOYSA-N
InChi: 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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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