Description
CNX-500 is a probe consisting of a covalent Btk inhibitor (CC-292) chemically linked to biotin. CNX-500 retains inhibitory activity against Btk (IC50 of 0.5 nM) and the ability to form a covalent bond with Btk. CNX-500 has low inhibitory effects on kinase epidermal growth factor receptor, and upstream Src-family kinases including Syk and Lyn.
Product information
CAS Number: 1202758-21-1
Molecular Weight: 961.18
Formula: C48H68N10O9S
Chemical Name: N-(3-{2-[2-(3-{5-[(3aS,4S,6aR)-2-oxo-hexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanamido}propoxy)ethoxy]ethoxy}propyl)-N'-(3-{3-[(5-methyl-4-{[3-(prop-2-enamido)phenyl]amino}pyrimidin-2-yl)amino]phenoxy}propyl)pentanediamide
Smiles: CC1=CN=C(NC2=CC(=CC=C2)OCCCNC(=O)CCCC(=O)NCCCOCCOCCOCCCNC(=O)CCCC[C@@H]2SC[C@@H]3NC(=O)N[C@H]23)N=C1NC1=CC(=CC=C1)NC(=O)C=C
InChiKey: SBOPEFHTOFMNSD-IAWMPOBQSA-N
InChi: InChI=1S/C48H68N10O9S/c1-3-41(59)53-35-12-6-13-36(30-35)54-46-34(2)32-52-47(58-46)55-37-14-7-15-38(31-37)67-25-11-22-51-44(62)19-8-18-43(61)50-21-10-24-65-27-29-66-28-26-64-23-9-20-49-42(60)17-5-4-16-40-45-39(33-68-40)56-48(63)57-45/h3,6-7,12-15,30-32,39-40,45H,1,4-5,8-11,16-29,33H2,2H3,(H,49,60)(H,50,61)(H,51,62)(H,53,59)(H2,56,57,63)(H2,52,54,55,58)/t39-,40-,45-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 50 mg/mL (52.02 mM; Need ultrasonic).
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:
Used in a competition assay, CNX-500 detects free, uninhibited Btk and is excluded from interaction with Btk previously bonded by CC-292. In Ramos cells exposed to a range of CC-292 concentrations, the amount of Btk captured by the probe is compared with untreated samples and the extent of Btk bonded is demonstrated to be proportional to CC-292 drug concentration.
Products are for research use only. Not for human use.
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