SJF620 is a PROTAC connected by ligands for Cereblon and Btk with a DC 50 of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN
In Vitro
SJF620 is a PROTAC that retains potent degradation of BTK in cellular assays with a DC 50 of 7.9 nM in Burkitt lymphoma cell line NAMALWA. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SJF620 has a super pharmacokinetic profile in mice (1 mg/kg; i.v.) with the half life (t 1/2 ) of 1.64 h. SJF620 exhibits a significantly better pharmacokinetic profile than MT802 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:Cereblon
Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Benzenoids |
| Classe | Benzene and substituted derivatives |
| Subclass | Diphenylethers |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Diphenylethers |
| Alternative Parents | Phenylpyrazoles Diarylethers Isoindolones Alpha amino acids and derivatives Pyrazolo[3,4-d]pyrimidines Isoindoles Piperidinediones Phenoxy compounds Phenol ethers Delta lactams Aminopyrimidines and derivatives Alkyl aryl ethers Imidolactams Tertiary carboxylic acid amides N-unsubstituted carboxylic acid imides Heteroaromatic compounds Dicarboximides Trialkylamines Dialkyl ethers Azacyclic compounds Primary amines Organopnictogen compounds Organic oxides Hydrocarbon derivatives Carbonyl compounds |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | Diphenylether - Phenylpyrazole - Diaryl ether - Isoindolone - Alpha-amino acid or derivatives - Pyrazolo[3,4-d]pyrimidine - Pyrazolopyrimidine - Isoindole or derivatives - Isoindole - Isoindoline - Phenoxy compound - Piperidinedione - Phenol ether - Piperidinone - Delta-lactam - Aminopyrimidine - Alkyl aryl ether - Imidolactam - Pyrimidine - Piperidine - Heteroaromatic compound - Tertiary carboxylic acid amide - Pyrazole - Carboxylic acid imide, n-unsubstituted - Dicarboximide - Carboxylic acid imide - Azole - Tertiary aliphatic amine - Tertiary amine - Lactam - Carboxamide group - Amino acid or derivatives - Azacycle - Organoheterocyclic compound - Ether - Dialkyl ether - Carboxylic acid derivative - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Organic oxide - Hydrocarbon derivative - Primary amine - Organooxygen compound - Organonitrogen compound - Carbonyl group - Amine - Aromatic heteropolycyclic compound |
| Descrição | This compound belongs to the class of organic compounds known as diphenylethers. These are aromatic compounds containing two benzene rings linked to each other through an ether group. |
| External Descriptors | Not available |
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Solubilidade | DMSO : 100 mg/mL (131.43 mM; Need ultrasonic) |
|---|---|
| Peso molecular | 760.800 g/mol |
| XLogP3 | 3.200 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 12 |
| Rotatable Bond Count | 15 |
| Exact Mass | 760.333 Da |
| Monoisotopic Mass | 760.333 Da |
| Topological Polar Surface Area | 176.000 Ų |
| Heavy Atom Count | 56 |
| Formal Charge | 0 |
| Complexity | 1310.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 1 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |
