Description
BSJ-03-123 is a Selective Cdk6 degrader. BSJ-03-123 exploits protein-interface determinants to achieve proteome-wide selectivity for the degradation of cyclin-dependent kinase 6 (CDK6). Pharmacologic CDK6 degradation targets a selective dependency of acute myeloid leukemia cells, and transcriptomics and phosphoproteomics profiling of acute degradation of CDK6 enabled dynamic mapping of its immediate role in coordinating signaling and transcription.
Product information
CAS Number: 2361493-16-3
Molecular Weight: 937.01
Formula: C47H56N10O11
Synonym:
BSJ
Chemical Name: N-[2-[2-[2-[2-[4-[6-[(6-Acetyl-8-cyclopentyl-7, 8-dihydro-5-methyl-7-oxopyrido[2, 3-d]pyrimidin-2-yl)amino]-3-pyridinyl]-1-piperazinyl]ethoxy]ethoxy]ethoxy]ethyl]-2-[[2-(2, 6-dioxo-3-piperidinyl)-2, 3-dihydro-1, 3-dioxo-1H-isoindol-4-yl]oxy]acetamide
Smiles: CC(=O)C1C(=O)N(C2CCCC2)C2=NC(NC3=CC=C(C=N3)N3CCN(CCOCCOCCOCCNC(=O)COC4=CC=CC5=C4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)=NC=C2C=1C
InChiKey: LUHCYAOYQIFNRN-UHFFFAOYSA-N
InChi: InChI=1S/C47H56N10O11/c1-29-34-27-50-47(53-42(34)56(31-6-3-4-7-31)45(63)40(29)30(2)58)51-37-12-10-32(26-49-37)55-17-15-54(16-18-55)19-21-66-23-25-67-24-22-65-20-14-48-39(60)28-68-36-9-5-8-33-41(36)46(64)57(44(33)62)35-11-13-38(59)52-43(35)61/h5,8-10,12,26-27,31,35H,3-4,6-7,11,13-25,28H2,1-2H3,(H,48,60)(H,52,59,61)(H,49,50,51,53)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO: 100 mg/mL(106.72 mM).
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:
BSJ-03-123 is a phthalimide-based degrader that exploits protein-interface determinants to achieve proteome-wide selectivity for the degradation of cyclin-dependent kinase 6 (CDK6). Pharmacologic CDK6 degradation targets a selective dependency of acute myeloid leukemia cells, and transcriptomics and phosphoproteomics profiling of acute degradation of CDK6 enabled dynamic mapping of its immediate role in coordinating signaling and transcription.
References:
- Matthias Brand, et al. Cell Chem Biol. 2019 Feb 21;26(2):300-306.e9.
Products are for research use only. Not for human use.
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