CAS NO: | 1532533-67-7 |
规格: | ≥98% |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
Molecular Weight (MW) | 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: (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one InChi Key: IUVCFHHAEHNCFT-INIZCTEOSA-N InChi Code: InChI=1S/C31H24F3N5O3/c1-15(2)41-24-9-7-18(12-22(24)34)27-26-30(35)36-14-37-31(26)39(38-27)16(3)29-25(17-5-4-6-19(32)11-17)28(40)21-13-20(33)8-10-23(21)42-29/h4-16H,1-3H3,(H2,35,36,37)/t16-/m0/s1 SMILES Code: O=C1C(C2=CC=CC(F)=C2)=C([C@@H](N3C4=NC=NC(N)=C4C(C5=CC=C(C(F)=C5)OC(C)C)=N3)C)OC6=CC=C(F)C=C16 |
Synonyms | RP 5264; RP-5264; TGR 1202; Umbralisib; TGR1202; TGR-1202; RP5264; |
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: Umbralisib (TGR-1202) is a novel PI3Kδ inhibitor, with IC50 and EC50 of 22.2 nM and 24.3 nM, respectively; Umbralisib (TGR-1202) is also active against CK1ε, with an EC50 value of 6.0 μM.
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. |