TGR-1202 hydrochloride
Modify Date: 2024-01-07 17:40:00
TGR-1202 hydrochloride structure
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Common Name | TGR-1202 hydrochloride | ||
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| CAS Number | 1532533-78-0 | Molecular Weight | 608.010 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C31H25ClF3N5O3 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of TGR-1202 hydrochlorideUmbralisib hydrochloride (TGR-1202 hydrochloride) is a novel PI3Kδ inhibitor, with IC50 and EC50 of 22.2 nM and 24.3 nM, respectively; Umbralisib hydrochloride (TGR-1202 hydrochloride) is also active against CK1ε, with an EC50 value of 6.0 μM. |
| Name | TGR-1202 hydrochloride |
|---|---|
| Synonym | More Synonyms |
| Description | Umbralisib hydrochloride (TGR-1202 hydrochloride) is a novel PI3Kδ inhibitor, with IC50 and EC50 of 22.2 nM and 24.3 nM, respectively; Umbralisib hydrochloride (TGR-1202 hydrochloride) is also active against CK1ε, with an EC50 value of 6.0 μM. |
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| Related Catalog | |
| Target |
PI3Kδ:22.2 nM (IC50) |
| 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 (TGR-1202; 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]. |
| 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 (TGR-1202; 150 mg/kg, daily p.o.) significantly shrinks the tumors by day 25[2]. |
| References |
| Molecular Formula | C31H25ClF3N5O3 |
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| Molecular Weight | 608.010 |
| Exact Mass | 607.159790 |
| 2-{(1S)-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 hydrochloride (1:1) |
| 4H-1-Benzopyran-4-one, 2-[(1S)-1-[4-amino-3-[3-fluoro-4-(1-methylethoxy)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-6-fluoro-3-(3-fluorophenyl)-, hydrochloride (1:1) |