Tankyrase-IN-2 |
| رقم الكتالوجGC37735 |
Tankyrase-IN-2 (المركب 5k) هو مثبط فعال ، انتقائي ، وفعال عن طريق الفم (IC50s من 10 و 7 و 710 نانومتر لـ TNKS1 و TNKS2 وكذلك PARP1 ، على التوالي)يحتوي Tankyrase-IN-2 على خصائص فيزيائية كيميائية وخصائص حركية دوائية تعدل نشاط مسار Wnt في نموذج طعم أجنبي للقولون والمستقيم
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1588870-36-3
Sample solution is provided at 25 µL, 10mM.
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Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model[1]. IC50: 10 nM (TNKS1), 7 nM (TNKS2), 710 nM (PARP1)[1]
Tankyrase-IN-2 (1-10000 nM; 24 hours) leads to a dose-dependent increase of tankyrase protein abundance with an EC50 of 320 nM in DLD1 cells. This is in the same potency range as the value for axin2 increase (EC50=319 nM)[1].
[1]. Buchstaller HP, et al. Discovery and Optimization of 2-Arylquinazolin-4-ones into a Potent and Selective TankyraseInhibitor Modulating Wnt Pathway Activity. J Med Chem. 2019 Aug 5.
Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)
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