A TNKS1 and TNKS2 inhibitor (IC50s = 0.014 and 0.010 µM

RK-287107 – 10 mg

Brand:
Cayman
CAS:
2171386-10-8
Storage:
-20
UN-No:
Non-Hazardous - /

RK-287107 is an inhibitor of the tankyrases TNKS1 and TNKS2 (IC50s = 0.014 and 0.010 µM, respectively).{60079} It is selective for TNKS1 and TNKS2 over poly(ADP-ribose) polymerase 1 (PARP1), PARP2, and PARP10 (IC50s = >20, 2.7, and 19.8 µM, respectively). RK-287107 inhibits Wnt-dependent signaling with an IC50 value of 0.077 µM in a reporter assay. It increases accumulation of Axin2, indicating inhibition of TNKS-mediated auto-PARsylation, in COLO 320DM colorectal cancer cells when used at a concentration of 0.1 µM. RK-287107 also inhibits cell growth in the same model (GI50 = 0.45 µM). It reduces tumor growth in a COLO 320DM mouse xenograft model when administered at a dose of 150 mg/kg twice per day.  

 

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SKU: 30998 - 10 mg Category:

Description

A TNKS1 and TNKS2 inhibitor (IC50s = 0.014 and 0.010 µM, respectively); selective for TNKS1 and TNKS2 over PARP1, PARP2, and PARP10 (IC50s = >20, 2.7, and 19.8 µM, respectively); inhibits Wnt-dependent signaling (IC50 = 0.077 µM in a reporter assay); increases Axin2 accumulation in COLO 320DM cells at 0.1 µM; inhibits cell growth in COLO 320DM cells (GI50 = 0.45 µM); reduces tumor growth in a COLO 320DM mouse xenograft model at 150 mg/kg

Formal name: 2-[4,6-difluoro-1-(2-hydroxyethyl)spiro[3H-indole-3,4′-piperidine]-1′(2H)-yl]-5,6,7,8-tetrahydro-4(3H)-quinazolinone

Synonyms: 

Molecular weight: 416.5

CAS: 2171386-10-8

Purity: ≥98%

Formulation: A solid

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