WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H122621
CAS#: N/A
Description: SKLB-03220 is a covalent EZH2 Inhibitor (IC50 = 1.72 nM) Based on Tazemetostat Scaffold for the Treatment of Ovarian Cancer. SKLB-03220 could covalently bind to the S-adenosylmethionine (SAM) pocket of EZH2. Besides, SKLB-03220 was highly potent for EZH2MUT, while exhibiting weak activities against other tested histone methyltransferases (HMTs) and kinases. Moreover, SKLB-03220 displayed noteworthy potency against ovarian cancer cell lines and continuously abolished H3K27me3 after washing out. Furthermore, oral administration of SKLB-03220 significantly inhibited tumor growth in PA-1 xenograft model without obvious adverse effects.
Hodoodo Cat#: H122621
Name: SKLB-03220
CAS#: N/A
Chemical Formula: C33H40N4O4
Exact Mass: 556.30
Molecular Weight: 556.710
Elemental Analysis: C, 71.20; H, 7.24; N, 10.06; O, 11.50
This product is not in stock, which may be available by custom synthesis.
For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge).
Quote less than 1g will not be provided. To request quote, please email to sales @hodoodo.com or click below button.
Note: Price will be listed if it is available in the future.
Synonym: SKLB-03220; SKLB 03220; SKLB03220
IUPAC/Chemical Name: 5'-acrylamido-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-2',4-dimethyl-[1,1'-biphenyl]-3-carboxamide
InChi Key: QKOGMESAENVJHH-UHFFFAOYSA-N
InChi Code: InChI=1S/C33H40N4O4/c1-7-31(38)36-25-10-9-20(3)27(18-25)24-16-28(32(39)34-19-29-21(4)15-22(5)35-33(29)40)23(6)30(17-24)37(8-2)26-11-13-41-14-12-26/h7,9-10,15-18,26H,1,8,11-14,19H2,2-6H3,(H,34,39)(H,35,40)(H,36,38)
SMILES Code: C=CC(NC1=CC=C(C)C(C2=CC(C(NCC3=C(C)C=C(C)NC3=O)=O)=C(C)C(N(C4CCOCC4)CC)=C2)=C1)=O
Appearance: To be determined
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:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 556.71 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 |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
Zhang Q, Chen X, Cao J, Yang W, Wan G, Feng Q, Zhou S, Yang H, Wang N, Liu Z, Xiao H, Zhu Y, Yu L. Discovery of a Novel Covalent EZH2 Inhibitor Based on Tazemetostat Scaffold for the Treatment of Ovarian Cancer. J Med Chem. 2023 Jan 24. doi: 10.1021/acs.jmedchem.2c01370. Epub ahead of print. PMID: 36692394.