MS154
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 533717

CAS#: 2550393-21-8

Description: MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon-binding moiety joined by a linker to gefitinib. MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50 values are 11 and 25 nM in HCC-827 and H3255 cells, respectively; Dmax > 95% at 50 nM), but not in WT-EGFR-bearing ovarian and lung cancer cells lines. It is bioavailable in mice following ip administration.

Chemical Structure

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MS154
CAS# 2550393-21-8
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 533717
Name: MS154
CAS#: 2550393-21-8
Chemical Formula: C46H54ClFN8O8
Exact Mass: 900.37
Molecular Weight: 901.434
Elemental Analysis: C, 61.29; H, 6.04; Cl, 3.93; F, 2.11; N, 12.43; O, 14.20

Price and Availability

Size Price Availability Quantity
5mg USD 750 2 Weeks
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Synonym: MS154; MS-154; MS 154;

IUPAC/Chemical Name: 3-(4-(3-((4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)propyl)piperazin-1-yl)-N-(8-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)octyl)propanamide

InChi Key: ALKKWBPMCDDKKA-UHFFFAOYSA-N

InChi Code: InChI=1S/C46H54ClFN8O8/c1-62-38-28-35-32(43(51-29-50-35)52-30-12-13-34(48)33(47)26-30)27-39(38)64-25-9-18-54-20-22-55(23-21-54)19-16-40(57)49-17-6-4-2-3-5-7-24-63-37-11-8-10-31-42(37)46(61)56(45(31)60)36-14-15-41(58)53-44(36)59/h8,10-13,26-29,36H,2-7,9,14-25H2,1H3,(H,49,57)(H,50,51,52)(H,53,58,59)

SMILES Code: O=C(NCCCCCCCCOC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCN4CCN(CCCOC5=CC6=C(NC7=CC=C(F)C(Cl)=C7)N=CN=C6C=C5OC)CC4

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

More Info:

Product Data:
Product Data
Instruction:
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Biological target: MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant epidermal growth factor receptor (EGFR).
In vitro activity: This study first examined the EGFR protein degradation induced by compounds 6 and 10 (MS154) in a wide range of concentrations. As illustrated in Figure 6, compounds 6 and 10 effectively reduced the mutant EGFR protein level in a concentration-dependent manner in both HCC-827 and H3255 cells. The CRBN-recruiting degrader 10 also inhibited the growth of H3255 cell, albeit it was not as potent as compound 6 and PROTAC3. Reference: J Med Chem. 2020 Feb 13;63(3):1216-1232. https://pubmed.ncbi.nlm.nih.gov/31895569/
In vivo activity: TBD

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 90.1 100.00

Preparing Stock Solutions

The following data is based on the product molecular weight 901.43 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.

Recalculate based on batch purity %
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
Formulation protocol: Cheng M, Yu X, Lu K, Xie L, Wang L, Meng F, Han X, Chen X, Liu J, Xiong Y, Jin J. Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders. J Med Chem. 2020 Feb 13;63(3):1216-1232. doi: 10.1021/acs.jmedchem.9b01566. Epub 2020 Jan 14. PMID: 31895569; PMCID: PMC7318554.
In vitro protocol: Cheng M, Yu X, Lu K, Xie L, Wang L, Meng F, Han X, Chen X, Liu J, Xiong Y, Jin J. Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders. J Med Chem. 2020 Feb 13;63(3):1216-1232. doi: 10.1021/acs.jmedchem.9b01566. Epub 2020 Jan 14. PMID: 31895569; PMCID: PMC7318554.
In vivo protocol: TBD

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1: Cheng M, Yu X, Lu K, Xie L, Wang L, Meng F, Han X, Chen X, Liu J, Xiong Y, Jin J. Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders. J Med Chem. 2020 Feb 13;63(3):1216-1232. doi: 10.1021/acs.jmedchem.9b01566. Epub 2020 Jan 14. PMID: 31895569; PMCID: PMC7318554.