WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H121013
CAS#: 2640723-72-2
Description: WB214 is a MDM2 degrader (IC50 = 1.2 nM). WB214 was identified as the most potent anti-proliferative agent in various leukemia cell lines. WB214 not only effectively induced the degradation of MDM2, but also led to the degradation of p53. Further studies revealed that WB214 degraded MDM2 as a molecular glue. Finally, it was found that WB214 could potently degrade GSPT1, which could rationalize the inhibition of cell growth.
Hodoodo Cat#: H121013
Name: WB214
CAS#: 2640723-72-2
Chemical Formula: C44H43ClF3N5O7
Exact Mass: 845.28
Molecular Weight: 846.300
Elemental Analysis: C, 62.45; H, 5.12; Cl, 4.19; F, 6.73; N, 8.28; O, 13.23
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Synonym: WB214; WB-214; WB 214
IUPAC/Chemical Name: ethyl 3-(2-(tert-butylamino)-1-(7-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)-N-(3,4,5-trifluorobenzyl)hept-6-ynamido)-2-oxoethyl)-6-chloro-1H-indole-2-carboxylate
InChi Key: WGGGBWUFPMJXRU-UHFFFAOYSA-N
InChi Code: InChI=1S/C44H43ClF3N5O7/c1-5-60-43(59)38-36(28-16-15-26(45)21-32(28)49-38)39(41(57)51-44(2,3)4)53(22-24-19-30(46)37(48)31(47)20-24)35(55)14-9-7-6-8-11-25-12-10-13-27-29(25)23-52(42(27)58)33-17-18-34(54)50-40(33)56/h10,12-13,15-16,19-21,33,39,49H,5-7,9,14,17-18,22-23H2,1-4H3,(H,51,57)(H,50,54,56)
SMILES Code: FC1=C(F)C(F)=CC(CN(C(CCCCC#CC2=CC=CC3=C2CN(C4CCC(NC4=O)=O)C3=O)=O)C(C5=C(C(OCC)=O)NC6=CC(Cl)=CC=C56)C(NC(C)(C)C)=O)=C1
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 846.30 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: |
Wang B, Liu J, Tandon I, Wu S, Teng P, Liao J, Tang W. Development of MDM2 degraders based on ligands derived from Ugi reactions: Lessons and discoveries. Eur J Med Chem. 2021 Jul 5;219:113425. doi: 10.1016/j.ejmech.2021.113425. Epub 2021 Apr 4. PMID: 33862513; PMCID: PMC8165035.