| Identification | Back Directory | [Name]
RK-287107 | [CAS]
2171386-10-8 | [Synonyms]
RK-287107
RK287107;RK 287107
4(3H)-Quinazolinone, 2-[4,6-difluoro-1-(2-hydroxyethyl)spiro[3H-indole-3,4'-piperidine]-1'(2H)-yl]-5,6,7,8-tetrahydro- | [Molecular Formula]
C22H26F2N4O2 | [MDL Number]
MFCD32062810 | [MOL File]
2171386-10-8.mol | [Molecular Weight]
416.46 |
| Chemical Properties | Back Directory | [Boiling point ]
602.5±65.0 °C(Predicted) | [density ]
1.48±0.1 g/cm3(Predicted) | [storage temp. ]
4°C, protect from light | [solubility ]
DMSO: soluble | [form ]
A solid | [pka]
14.24±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
RK-287107 is a potent and specific tankyrase inhibitor with IC50s of 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively. RK-287107 blocks colorectal cancer cell growth[1]. | [in vivo]
RK-287107 (100 and 300 mg/kg; i.p. administration; once per day; 5-days on/ 2-days off schedule for 2 weeks) inhibits tumor growth in a mouse xenograft model[1]. | Animal Model: | 6-week-old female NOD.CB17-Prkdcscid/J mice with colorectal cancer COLO-320DM[1] | | Dosage: | 100 and 300 mg/kg | | Administration: | Administration i.p.; once per day; 5-days on/ 2-days off schedule for 2 weeks | | Result: | 100 and 300 mg/kg resulted in 32.9% and 44.2% TGI, respectively. |
| [IC 50]
tankyrase-1: 14.3 nM (IC50); tankyrase-2: 10.6 nM (IC50) | [References]
[1] Mizutani A, et al. RK-287107, a potent and specific tankyrase inhibitor, blocks colorectal cancer cell growth in a preclinical model. Cancer Sci. 2018 Dec;109(12):4003-4014. DOI:10.1111/cas.13805 |
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