DC Chemicals Limited
China
Product Name: TGR-1202(Umbralisib)
Price: $800.0/100mg $1350.0/250mg $2700.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

1532533-67-7

1532533-67-7 structure

1532533-67-7 structure

Name: tgr-1202
Chemical Name: tgr-1202
CAS Number: 1532533-67-7
Molecular Formula: C₃₁H₂₄F₃N₅O₃
Molecular Weight: 571.54900
Catalog: Research Areas Cancer
Create Date: 2017-11-10 09:55:43
Modify Date: 2024-01-14 22:17:07
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.

Name	tgr-1202
Synonyms	(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

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.
Related Catalog	Research Areas >> Cancer
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 (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].
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].
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

Melting Point	139 - 142 °C
Molecular Formula	C₃₁H₂₄F₃N₅O₃
Molecular Weight	571.54900
Exact Mass	571.18300
PSA	109.06000
LogP	7.24390
Storage condition	-20℃