2171386-10-8
2171386-10-8 structure
- Name: RK-287107
- Chemical Name: RK-287107
- CAS Number: 2171386-10-8
- Molecular Formula: C22H26F2N4O2
- Molecular Weight: 416.46
- Catalog: Signaling Pathways Cell Cycle/DNA Damage PARP
- Create Date: 2019-06-01 17:20:34
- Modify Date: 2025-09-18 16:44:05
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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].
| Name | RK-287107 |
|---|
| Description | 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]. |
|---|---|
| Related Catalog | |
| Target |
tankyrase-1:14.3 nM (IC50) tankyrase-2:10.6 nM (IC50) |
| 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[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]. Cell Proliferation Assay[1] 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[1] 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 |
| 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. |
| References |
| Molecular Formula | C22H26F2N4O2 |
|---|---|
| Molecular Weight | 416.46 |