product name TGR-1202
Description: TGR-1202 (also known as RP5264) is a novel PI3Kδ inhibitor, with IC50 and EC50 of 22.2 nM and 24.3 nM, respectively; Also active against CK1ε, with an EC50 value of 6.0 μM. It 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.
References: Blood. 2017 Jan 5;129(1):88-99; Swaroop Vakkalanka, et al. AACR Poster. 2012, Poster3741.
571.55
Formula
C31H24F3N5O3
CAS No.
1532533-67-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (175 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: 7 mg/mL (12.2 mM)
Solubility (In vivo)
Chemical Name
RP5264
other peoduct :
| In Vitro |
In vitro Activity: TGR-1202 causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM. In human lymphoma and leukemia cell lines, TGR-1202 (10 nM-100 μM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner. TGR-1202 and carfilzomib synergistically kill blood cancer cells through disrupting the 4E-BP1-eIF4F-c-Myc axis. TGR-1202 and carfilzomib in combination synergistically and selectively silence the c-Myc and E2F transcription programs. TGR-1202 (15-50 μM) potently represses the expression of c-Myc in the DLBCL cell line LY7, and is uniquely characterized with structural features suitable for targeting CK1ε in lymphoma cells. Kinase Assay: Cell Assay: Multiple Myeloma resistant (MM-1R) or sensitive (MM-1S) cells are incubated with desired concentrations of RP5264. Growth is assessed after 96 h by a MTT assay. |
|---|---|
| In Vivo | In a subcutaneous xenograft model of T-cell acute lymphoblastic leukemia (T-ALL) in NOD/SCID mice using the MOLT-4 cell line, TGR-1202 (150 mg/kg, daily p.o.) significantly shrinks the tumors by day 25 |
| Animal model | Female Balb/c mice |
| Formulation & Dosage | 12.5, 25, 50 mg/kg; oral gavage |
| References | Blood. 2017 Jan 5;129(1):88-99; Swaroop Vakkalanka, et al. AACR Poster. 2012, Poster3741. |
