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| Cas No.: | 1532533-67-7 |
| Chemical Name: | Umbralisib |
| Synonyms: | RP5264; TGR1202; TGR 1202; RP-5264; RP 5264 |
| SMILES: | O=C1C2C(=CC=C(C=2)F)OC(C(C)N2C3C(=C(N=CN=3)N)C(C3C=C(F)C(OC(C)C)=CC=3)=N2)=C1C1C=C(F)C=CC=1 |
| Formula: | C31H24F3N5O3 |
| M.Wt: | 571.56 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | 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. |
| Target: | PI3Kδ:22.2 nM (IC50) |
| 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, Umbralisib (RP5264; 150 mg/kg, daily p.o.) significantly shrinks the tumors by day 25[2]. |
| In Vitro: | Umbralisib (RP5264) causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM[1]. In human lymphoma and leukemia cell lines, Umbralisib (RP5264; 10 nM-100 μM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner. Umbralisib and carfilzomib synergistically kill blood cancer cells through disrupting the 4E-BP1-eIF4F-c-Myc axis. Umbralisib and carfilzomib in combination synergistically and selectively silence the c-Myc and E2F transcription programs. Umbralisib (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[2]. |
| References: | [1]. Swaroop Vakkalankaa, et al. Inhibition of PI3Kδ kinase by a selective, small molecule inhibitor suppresses B-cell proliferation and leukemic cell growth. [2]. Deng C, et al. Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies. Blood. 2017 Jan 5;129(1):88-99 |