RK-287107
RK-287107 Basic information
- Product Name:
- RK-287107
- 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-
- inhibit,poly ADP ribose polymerase,RK287107,RK-287107,PARP,RK 287107,Inhibitor
- RK-287107, 10 mM in DMSO
- RK-287107 ，S8876
- CAS:
- 2171386-10-8
- MF:
- C22H26F2N4O2
- MW:
- 416.46
- Mol File:
- 2171386-10-8.mol
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RK-287107 Chemical Properties
- 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
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RK-287107 Usage And Synthesis
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
RK-287107Supplier
Shanghai Lollane Biological Technology Co.,Ltd.
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- 021-52996696，15000506266 15000506266
Shanghai EFE Biological Technology Co., Ltd.
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- 021-65675885 18964387627
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Shanghai YuanYe Biotechnology Co., Ltd.
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- 021-61312847; 18021002903
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ShangHai Biochempartner Co.,Ltd
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Shanghai Chaolan Chemical Technology Center
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