Dezapelisib
Dezapelisib (NCB040093) is a potent inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ). Dezapelisib is a promising research strategy for select R/R B-cell lymphomas.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 1262440-25-4
- Formel: C20H16FN7OS
- Molecular Weight:421.45
-
Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| B-cell | IC50 |
<0.05 μM
Compound: 67
|
Inhibition of PI3Kdelta in B-cells by proliferation assay
Inhibition of PI3Kdelta in B-cells by proliferation assay
|
[PMID: 22924688] |
| Pfeiffer | IC50 |
14 nM
Compound: 3; INCB040093
|
Cytotoxicity against human Pfeiffer cells assessed as reduction in cell viability incubated for 4 days by [3H]-thymidine incorporation based liquid scintillation counter method
Cytotoxicity against human Pfeiffer cells assessed as reduction in cell viability incubated for 4 days by [3H]-thymidine incorporation based liquid scintillation counter method
|
[PMID: 31749910] |
| Pfeiffer | IC50 |
66 nM
Compound: 3; INCB040093
|
Cytotoxicity against human Pfeiffer cells assessed as reduction in protein binding adjusted cell viability incubated for 4 days by [3H]-thymidine incorporation based liquid scintillation counter method
Cytotoxicity against human Pfeiffer cells assessed as reduction in protein binding adjusted cell viability incubated for 4 days by [3H]-thymidine incorporation based liquid scintillation counter method
|
[PMID: 31749910] |
| Sf21 | IC50 |
3751 nM
Compound: Dezapelisib
|
Inhibition of human full length recombinant N-terminal His-tagged PI3Kbeta/p85alpha expressed in baculovirus infected Sf21 insect cells
Inhibition of human full length recombinant N-terminal His-tagged PI3Kbeta/p85alpha expressed in baculovirus infected Sf21 insect cells
|
[PMID: 30530193] |
| SU-DHL-6 | IC50 |
18 nM
Compound: 3; INCB040093
|
Cytotoxicity against human SUDHL6 cells assessed as reduction in cell viability incubated for 4 days by celltiter glo luminescent assay
Cytotoxicity against human SUDHL6 cells assessed as reduction in cell viability incubated for 4 days by celltiter glo luminescent assay
|
[PMID: 31749910] |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS. Nr. 1262440-25-4
-
Molecular Weight 421.45
-
Formel C20H16FN7OS
-
SMILES
C[C@@H](C1=C(C2=CC(F)=CC=C2)C(N3C(SC=C3C)=N1)=O)NC4=C5C(N=CN5)=NC=N4
-
Synonyms
INCB040093
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)