Thalidomide-NH-PEG4-Ms

Thalidomide-NH-PEG4-Ms is an E3 ligase ligand-linker conjugate that incorporates Thalidomide based cereblon ligand and a linker used for PROTAC BCL-XL degrader XZ739.

Product information

CAS Number: 2140807-24-3

Molecular Weight: 527.54

Formula: C22H29N3O10S

Chemical Name: 2-{2-[2-(2-{[2-(2, 6-dioxopiperidin-3-yl)-1, 3-dioxo-2, 3-dihydro-1H-isoindol-4-yl]amino}ethoxy)ethoxy]ethoxy}ethyl methanesulfonate

Smiles: CS(=O)(=O)OCCOCCOCCOCCNC1=CC=CC2=C1C(=O)N(C1CCC(=O)NC1=O)C2=O

InChiKey: XWJKHOILPWWTDG-UHFFFAOYSA-N

InChi: InChI=1S/C22H29N3O10S/c1-36(30,31)35-14-13-34-12-11-33-10-9-32-8-7-23-16-4-2-3-15-19(16)22(29)25(21(15)28)17-5-6-18(26)24-20(17)27/h2-4,17,23H,5-14H2,1H3,(H,24,26,27)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

XZ739, a CRBN-dependent PROTAC BCL-XL degrader with a DC50 value of 2.5 nM in MOLT-4 cells after 16 h treatment. XZ739 also induces cell death through caspase-mediated apoptosis.

References:

1. Xuan Zhang,et al. Discovery of PROTAC BCL-X L Degraders as Potent Anticancer Agents With Low On-Target Platelet Toxicity. Eur J Med Chem. 2020 Apr 15;192:112186.

Products are for research use only. Not for human use.