umbralisib (TGR-1202) (C007B-304843)

InformationUmbralisib (TGR-1202, Rp-5264), a novel, next generationPI3Kδinhibitor, inhibits PI3Kδ activity in enzyme and cell based assays withIC50andEC50values of 22.2 & 24.3 nM, respectively.TargetsPI3Kδ (Cell-free assay) 22.2 nMIn vitroThe compound displays a high degree of selectivity over the alpha (>1000 fold), beta (>30-50 fold), and gamma (>15-50 fold) isoforms. Additionally, the compound causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM. Treatment of PBMC with RP5264 results initially in a G2/M arrest followed by subsequent increase in the number of Sub G0 cells. Viability assays demonstrate that the compound causes a significant inhibition in growth as well as Akt phosphorylation of immortalized and primary leukemic cells.In vivoThe compound exhibits good oral absorption with favourable pharmacokinetic properties in rodents. It also has an excellent safety profile.Cell Research(from reference)Cell lines：Multiple Myeloma resistant (MM-1R) or sensitive (MM-1S) cells Incubation Time：96 h. Specification: 0.99 Molecular Formula: C31H24F3N5O3 Molecular Weight: 571.55 PubChem CID: 72950888 Isomeric SMILES: C[C@@H](C1=C(C(=O)C2=C(O1)C=CC(=C2)F)C3=CC(=CC=C3)F)N4C5=NC=NC(=C5C(=N4)C6=CC(=C(C=C6)OC(C)C)F)N

UPC:

51111745

Condition:

New

Weight:

0.96 Ounces

HazmatClass:

No

WeightUOM:

LB

MPN:

U413938-10mg

CAS:

1532533-67-7

Product Size:

10mg