RK-287107

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

RK-287107 是一种有效且特异性的坦科聚合酶抑制剂（坦科聚合酶 1 和坦科聚合酶 2 的 IC50 分别为 14.3 和 10.6 nM）。

RK-287107 is an effective and specific inhibitor of tankyrase (IC50s: 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively).

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. Cell Proliferation Assay Cell Line:Colorectal cancer COLO-320DM, SW403, RKO, HCC2998, HCT-116, and DLD-1 cells Concentration:0.01, 0.1, 1, 10 μM Incubation Time:12 hours 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. Western Blot Analysis Cell Line:COLO-320DM cells Concentration:0.03, 0.1, 0.33, 1, 3, and 10 μM Incubation Time:16 hours Result:Downregulation of active β-catenin was observed

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. Animal Model:6-week-old female NOD.CB17-Prkdcscid/J mice with colorectal cancer COLO-320DM 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.

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Others

Other Targets

tankyrase 1|tankyrase 2

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2171386-10-8

416.46

C22H26F2N4O2

>98% (HPLC)

DMSO:120 mg/mL (288.14 mM; Need ultrasonic)

OCCN(C1)c2cc(F)cc(F)c2C1(CC1)CCN1C(N1)=NC(CCCC2)=C2C1=O

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(-20℃)

With Ice Pack

≥ 2 years