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RK-287107 | PARP 抑制剂 | MCE
请完善您的信息,提交审核升级会员,查看RK-287107的详细信息 完成审核- 升级您的专属账户 即刻兑换价值 500 积分的多种礼券 根据当地政策法规的要求,该产品仅对科研客户提供相关信息。 您需要登录/注册您的专属账户,或与客服人员直接联系 确认您的产品用途,通过审核后,即可查看MCE会员专属产品。 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。 1.客户无需承担相应的运输费用。 2.同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内 可免费申领三个不同产品的试用装。 3.试用装只面向终端客户。 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]. 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[1]. RK-287107 (0.03-10 μM; 16 hours) causes accumulation of tankyrase and Axin1/2[1]. RK-287107 (0.03-10 μM; 16 hours) also downregulates β-catenin signaling in cultured cells[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Line: Colorectal cancer COLO-320DM, SW403, RKO, HCC2998, HCT-116, and DLD-1 cells Result: Inhibited the growth of APC-mutated (β-catenin-dependent) colorectal cancer COLO-320DM and SW403 cells. The GI50 value of RK-287107 on COLO-320DM is 0.449 μM. Did not inhibit the growth of APC-wild (β-catenin-independent) colorectal cancer cell lines, including RKO, HCT-116, HCC2998 and DLD-1. 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-week-old female NOD.CB17-Prkdcscid/J mice with colorectal cancer COLO-320DM[1] Administration: Administration i.p.; once per day; 5-days on/ 2-days off schedule for 2 weeks 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 请依序添加每种溶剂:10% DMSO40% PEG3005% Tween-8045% salineSolubility: ≥ 2.08 mg/mL (4.99 mM); Clear solution 此方案可获得 ≥ 2.08 mg/mL (4.99 mM,饱和度未知) 的澄清溶液。以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液 请依序添加每种溶剂:10% DMSO90% (20% SBE-β-CD in saline)Solubility: ≥ 2.08 mg/mL (4.99 mM); Clear solution 此方案可获得 ≥ 2.08 mg/mL (4.99 mM,饱和度未知) 的澄清溶液。以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明 请依序添加每种溶剂:10% DMSO90% corn oilSolubility: ≥ 2.08 mg/mL (4.99 mM); Clear solution 此方案可获得 ≥ 2.08 mg/mL (4.99 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 Keywords: RK-287107RK287107RK 287107PARPpoly ADP ribose polymeraseInhibitorinhibitorinhibit Please fill out this form to request the QC report. We will send it to your Email address shortly. Your information is safe with us. * Required Fields. MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务,不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。 站点地图 隐私声明