WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 408052
CAS#: Unknown
Description: MS432 is a highly selective MEK1/2 degrader with IC50=31 nM. MS432 potently and selectively degraded MEK1 and MEK2 in a VHL E3 ligase- and proteasome-dependent manner and suppressed ERK phosphorylation in cells. MS432 was highly selective for MEK1/2 in global proteomic profiling studies. It was also bioavailable in mice and can be used for in vivo efficacy studies. MS432 potently reduced MEK1/2 protein levels and inhibited ERK signaling, and suppressed cancer cell proliferation effectively. MS432 displayed good plasma exposure in mice and can be used in the in vivo efficacy studies.
MedKoo Cat#: 408052
Name: MS432
CAS#: Unknown
Chemical Formula: C50H65F3IN7O6S
Exact Mass: 1075.3714
Molecular Weight: 1076.0727
Elemental Analysis: C, 55.81; H, 6.09; F, 5.30; I, 11.79; N, 9.11; O, 8.92; S, 2.98
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Synonym: MS432; MS-432; MS 432;
IUPAC/Chemical Name: (2S,4R)-1-((S)-20-(tert-Butyl)-1-(3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)phenyl)-1,18-dioxo-3-oxa-2,7,19-triazahenicosan-21-oyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)-ethyl)pyrrolidine-2-carboxamide
InChi Key: KCBAMQOKOLXLOX-BSZYMOERSA-N
InChi Code: 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
SMILES Code: O=C([C@H]1C[C@H](CN1C([C@H](C(C)(C)C)NC(CCCCCCCCCCNCCCONC(C2=CC=C(F)C(F)=C2NC3=CC=C(I)C=C3F)=O)=O)=O)O)N[C@H](C4=CC=C(C5=C(C)N=CS5)C=C4)C
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 1076.0727 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Wei J, Hu J, Wang L, Xie L, Jin MS, Chen X, Liu J, Jin J. Discovery of a
First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader. J Med Chem.
2019 Nov 27. doi: 10.1021/acs.jmedchem.9b01528. [Epub ahead of print] PubMed
PMID: 31730343.
MEK1 and MEK2 (also known as MAP2K1 and MAP2K2) are the “gatekeepers” of the ERK signaling output with redundant roles in controlling ERK activity. Numerous inhibitors targeting MEK1/2 have been developed including three FDA-approved drugs. However, acquired resistance to MEK1/2 inhibitors has been observed in patients, and new therapeutic strategies are needed to overcome the resistance.
