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MedKoo Cat#: 464430 | Name: MS 154N
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Description:

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

MS 154N is a negative control for MS 154. The compound exhibits high binding-affinity for WT and L858R-mutant EGFR (Kd values are 3 and 4.3 nM, respectively), but does not significantly induce degradation of EGFR mutants.

Chemical Structure

MS 154N
MS 154N
CAS#unknown

Theoretical Analysis

MedKoo Cat#: 464430

Name: MS 154N

CAS#: unknown

Chemical Formula: C47H56ClFN8O8

Exact Mass: 914.3894

Molecular Weight: 915.46

Elemental Analysis: C, 61.66; H, 6.17; Cl, 3.87; F, 2.08; N, 12.24; O, 13.98

Price and Availability

Size Price Availability Quantity
5mg USD 750.00 2 Weeks
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Related CAS #
No Data
Synonym
MS 154N; MS154N; MS-154N;
IUPAC/Chemical Name
3-(4-(3-((4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)propyl)piperazin-1-yl)-N-(8-((2-(1-methyl-2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)octyl)propanamide
InChi Key
XFUDPXQGWCYCCR-UHFFFAOYSA-N
InChi Code
InChI=1S/C47H56ClFN8O8/c1-54-42(59)16-15-37(46(54)61)57-45(60)32-11-9-12-38(43(32)47(57)62)64-25-8-6-4-3-5-7-18-50-41(58)17-20-56-23-21-55(22-24-56)19-10-26-65-40-28-33-36(29-39(40)63-2)51-30-52-44(33)53-31-13-14-35(49)34(48)27-31/h9,11-14,27-30,37H,3-8,10,15-26H2,1-2H3,(H,50,58)(H,51,52,53)
SMILES Code
COC1=CC2=C(C=C1OCCCN3CCN(CCC(NCCCCCCCCOC4=C5C(N(C6CCC(N(C6=O)C)=O)C(C5=CC=C4)=O)=O)=O)CC3)C(NC7=CC(Cl)=C(F)C=C7)=NC=N2
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
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
View handling instruction
Biological target:
MS 154N is a negative control for MS 154.
In vitro activity:
The degraders 6 and 10 (MS 154) also potently inhibited the EGFR autophosphorylation (p-EGFR) and AKT phosphorylation (p-AKT), which is a downstream target of EGFR signaling pathway, in both cell lines. This study observed that the VHL-recruiting degrader 6 displayed slightly better EGFR degradation and downstream signaling inhibition effects than the CRBN-recruiting degrader 10 in HCC-827 cells, and the difference was more significant in H3255 cells. Reference: J Med Chem. 2020 Feb 13;63(3):1216-1232. https://pubmed.ncbi.nlm.nih.gov/31895569/
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMSO 91.6 100.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 915.46 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