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

Theoretical Analysis

MedKoo Cat#: 533717
Name: MS154
CAS#: 2550393-21-8
Chemical Formula: C46H54ClFN8O8
Exact Mass: 900.3737
Molecular Weight: 901.4344
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
5.0mg USD 530.0 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

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 90.14 100.0

Preparing Stock Solutions

The following data is based on the product molecular weight 901.4344 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

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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.

MS154

5.0mg / USD 530.0