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2171386-10-8

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2171386-10-8 Structure

2171386-10-8 Structure
IdentificationBack 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 PropertiesBack 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
Safety DataBack Directory
[Symbol(GHS) ]

Exclamation Mark (GHS07)
GHS07
[Signal word ]

Warning
Hazard InformationBack 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
Spectrum DetailBack Directory
[Spectrum Detail]

RK-287107(2171386-10-8)1HNMR
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