MedKoo Cat#: 464924 | Name: YM281

Description:

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

YM281 is a proteolysis-target chimera (PROTAC)-based EZH2 degrader. YM281 induced robust cell viability inhibition in diffuse large B-cell lymphoma (DLBCL) and other subtypes of lymphomas, outperforming a clinically used EZH2 inhibitor EPZ6438 (tazemetostat) that was only effective against DLBCL. The EZH2 degrader displayed promising antitumor activities in lymphoma xenografts and patient-derived primary.

Chemical Structure

YM281
YM281
CAS#2230914-84-6

Theoretical Analysis

MedKoo Cat#: 464924

Name: YM281

CAS#: 2230914-84-6

Chemical Formula: C56H71N7O9S

Exact Mass: 1017.5034

Molecular Weight: 1018.28

Elemental Analysis: C, 66.05; H, 7.03; N, 9.63; O, 14.14; S, 3.15

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
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Synonym
YM281; YM 281; YM-281;
IUPAC/Chemical Name
(2S,4R)-1-((S)-2-(2-(3-((3'-(((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)carbamoyl)-5'-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4'-methyl-[1,1'-biphenyl]-4-yl)oxy)propoxy)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
InChi Key
HBGYJNIDFUPUJQ-DDGSYWGGSA-N
InChi Code
InChI=1S/C56H71N7O9S/c1-9-62(42-19-23-70-24-20-42)47-27-41(26-45(36(47)4)52(66)58-30-46-34(2)25-35(3)60-53(46)67)39-15-17-44(18-16-39)72-22-10-21-71-32-49(65)61-51(56(6,7)8)55(69)63-31-43(64)28-48(63)54(68)57-29-38-11-13-40(14-12-38)50-37(5)59-33-73-50/h11-18,25-27,33,42-43,48,51,64H,9-10,19-24,28-32H2,1-8H3,(H,57,68)(H,58,66)(H,60,67)(H,61,65)/t43-,48+,51-/m1/s1
SMILES Code
CC(N1)=CC(C)=C(CNC(C2=CC(C3=CC=C(OCCCOCC(N[C@@H](C(C)(C)C)C(N4[C@H](C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)C[C@@H](O)C4)=O)=O)C=C3)=CC(N(CC)C7CCOCC7)=C2C)=O)C1=O
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

Preparing Stock Solutions

The following data is based on the product molecular weight 1,018.28 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
1: Tu Y, Sun Y, Qiao S, Luo Y, Liu P, Jiang ZX, Hu Y, Wang Z, Huang P, Wen S. Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma. J Med Chem. 2021 Jul 1. doi: 10.1021/acs.jmedchem.1c00460. Epub ahead of print. PMID: 34196564.