Pomalidomide-amido-C1-Br


Catalog No. Size PriceQuantity
M13185-2 Contact sales@xcessbio.com for quotation $100
M13185-10 Contact sales@xcessbio.com for quotation $100

Description

Pomalidomide-amido-C1-Br is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-amido-C1-Br can be used to design a B-Raf PROTAC degrader PROTAC B-Raf degrader 1 (HY-111758). PROTAC B-Raf degrader 1 has anti-cancer activity.

Product information

CAS Number: 2351106-38-0

Molecular Weight: 394.18

Formula: C15H12BrN3O5

Chemical Name: 2-bromo-N-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]acetamide

Smiles: O=C1CCC(C(=O)N1)N1C(=O)C2C=CC=C(NC(=O)CBr)C=2C1=O

InChiKey: VFHGCZZAGNKHIX-UHFFFAOYSA-N

InChi: InChI=1S/C15H12BrN3O5/c16-6-11(21)17-8-3-1-2-7-12(8)15(24)19(14(7)23)9-4-5-10(20)18-13(9)22/h1-3,9H,4-6H2,(H,17,21)(H,18,20,22)

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:

Pomalidomide-amido-C1-Br (Compound 6) can be used to design a B-Raf PROTAC degrader PROTAC B-Raf degrader 1 (Compound 2). PROTAC B-Raf degrader 1 can effectively kill cancer cells via inducing cells apoptosis. As a B-Raf degrader, PROTAC B-Raf degrader 1 can accelerate the degradation of B-Raf by recruiting ubiquitin-proteasome system, and further affects the expression of Mcl-1, a downstream protein of B-Raf.

References:

  1. Chen H, et al. Pomalidomide hybrids act as proteolysis targeting chimeras: Synthesis, anticancer activity and B-Raf degradation. Bioorg Chem. 2019 Jun;87:191-199.

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

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