RK-287107|2171386-10-8|-陌孚医药/Medlife

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RK-287107

目录号: PL08901 纯度: ≥99%

CAS No. :2171386-10-8

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中文名称	RK-287107
中文别名	化合物RK-287107;2-(4,6-二氟-1-(2-羟乙基)螺[二氢吲哚-3,4'-哌啶]-1'-基)-5,6,7,8-四氢喹唑啉-4(3H)-酮
英文名称	RK-287107
英文别名	2-(4,6-difluoro-1-(2-hydroxyethyl)spiro[indoline-3,4'-piperidin]-1'-yl)-5,6,7,8-tetrahydroquinazolin-4(3H)-one;GTPL10673;BCP30401;ZB1535;RK287107;RK 287107; RK287107;2-[4,6-difluoro-1-(2-hydroxyethyl)spiro[2H-indole-3,4'-piperidine]-1'-yl]-5,6,7,8-tetrahydro-3H-quinazolin-4-one;CID 137701512;RK-287107;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
Cas No.	2171386-10-8
分子式	C₂₂H₂₆F₂N₄O₂
分子量	416.46
包装储存	4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

产品详情	RK-287107 是一种有效的特异性 tankyrase 抑制剂，抑制 tankyrase-1 和 tankyrase-2，IC₅₀ 分别为 14.3 和 10.6 nM。RK-287107 可阻断结直肠癌细胞生长。
生物活性	RK-287107 is a potent and specific tankyrase inhibitor with IC 50 s of 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively. RK-287107 blocks colorectal cancer cell growth.
性状	Solid
IC50 & Target[1][2]	tankyrase-1 14.3 nM (IC50) tankyrase-2 10.
体外研究(In Vitro)	RK-87107 (0.01-10 μM; 12 hours) shows an antiproliferative effect on colorectal cancer cells harboring short adenomatous polyposis coli (APC) mutations. The 50% growth inhibition (GI50) value of RK-287107 on COLO-320DM cells is 0.449 μM. RK-287107 (0.03-10 μM; 16 hours) causes accumulation of tankyrase and Axin1/2. RK-287107 (0.03-10 μM; 16 hours) also downregulates β-catenin signaling in cultured cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献	[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.

溶解度数据	In Vitro: DMSO : 125 mg/mL (300.15 mM; Need ultrasonic)配制储备液

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