TGR-1202 hydrochloride

Modify Date: 2024-01-07 17:40:00

TGR-1202 hydrochloride structure	Common Name	TGR-1202 hydrochloride
	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 hydrochloride

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.

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.
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 (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	[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

Molecular Formula	C₃₁H₂₅ClF₃N₅O₃
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)

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

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Price: $132/5mg

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TGR-1202 hydrochloride

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