MS432 is a first-in-class and highly selective PD0325901-based VHL-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.

Product information

Molecular Weight: 1076.06

Formula: C50H65F3IN7O6S

Chemical Name: (2S, 4R)-1-[(2S)-2-[11-[3-[[3, 4-difluoro-2-(2-fluoro-4-iodoanilino)benzoyl]amino]oxypropylamino]undecanoylamino]-3, 3-dimethylbutanoyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-1, 3-thiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide

Smiles: CC1N=CSC=1C1C=CC(=CC=1)[C@H](C)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](NC(=O)CCCCCCCCCCNCCCONC(=O)C1=CC=C(F)C(F)=C1NC1=CC=C(I)C=C1F)C(C)(C)C

InChiKey: KCBAMQOKOLXLOX-BSZYMOERSA-N

InChi: InChI=1S/C50H65F3IN7O6S/c1-31(33-16-18-34(19-17-33)45-32(2)56-30-68-45)57-48(65)41-28-36(62)29-61(41)49(66)46(50(3,4)5)59-42(63)15-12-10-8-6-7-9-11-13-24-55-25-14-26-67-60-47(64)37-21-22-38(51)43(53)44(37)58-40-23-20-35(54)27-39(40)52/h16-23,27,30-31,36,41,46,55,58,62H,6-15,24-26,28-29H2,1-5H3,(H,57,65)(H,59,63)(H,60,64)/t31-,36+,41-,46+/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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).

In Vivo:

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.

Products are for research use only. Not for human use.