MS432 |
| رقم الكتالوجGC64292 |
MS432 هو أول من نوعه في فئته وانتقائي للغاية PD0325901 القائم على فون هيبل لينداو - تجنيد ديجريدر PROTAC لـ MEK1 و MEK2يعرض MS432 تعرضًا جيدًا للبلازما في الفئران ، حيث تظهر قيم DC50 تبلغ 31 نانومتر و 17 نانومتر لـ MEK1 و MEK2 في خلايا HT29 على التوالي
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2672512-44-4
Sample solution is provided at 25 µL, 10mM.
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MS432 is a first-in-class and highly selective PD0325901-based von Hippel-Lindau-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively[1].
MS432 (compound 23) is potent in reducing MEK1/2 protein levels in COLO 205 cells (DC50 (MEK1) = 18 ± 7 nM, DC50 (MEK2) = 11 ± 2 nM) and UACC257 cells (DC50 (MEK1) = 56 ± 25 nM, DC50 (MEK2) = 27 ± 19 nM).
MS432 (compound 23) displays good plasma exposure, which is approximately 3 to 20-fold higher than the GI50 values of compound 23 in the tested cancer cell lines[1].
[1]. Wei J, et al. Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader. J Med Chem. 2019 Dec 12;62(23):10897-10911.
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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