tgr-1202

Modify Date: 2025-08-21 15:24:53

tgr-1202 structure	Common Name	tgr-1202
	CAS Number	1532533-67-7	Molecular Weight	571.54900
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₃₁H₂₄F₃N₅O₃	Melting Point	139 - 142 °C
	MSDS	N/A	Flash Point	N/A

Use of tgr-1202

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
Synonym	More Synonyms

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
InChIKey	IUVCFHHAEHNCFT-INIZCTEOSA-N
SMILES	CC(C)Oc1ccc(-c2nn(C(C)c3oc4ccc(F)cc4c(=O)c3-c3cccc(F)c3)c3ncnc(N)c23)cc1F
Storage condition	-20℃

Name: Thermal Shift Assay. Domain: start/stop: M626-G746
Source: ChEMBL
Target: Peregrin
External Id: CHEMBL5062280

Name: Selectivity ratio of IC50 for PI3Kbeta (unknown origin) to IC50 for PI3Kdelta (unknow...
Source: ChEMBL
Target: N/A
External Id: CHEMBL4351080

Name: Selectivity ratio of IC50 for PI3Kalpha (unknown origin) to IC50 for PI3Kdelta (unkno...
Source: ChEMBL
Target: N/A
External Id: CHEMBL4351079

Name: Cytotoxicity against human PBMC assessed as reduction in cell viability at 2.5 to 5 u...
Source: ChEMBL
Target: N/A
External Id: CHEMBL5720100

Name: Primary qHTS for inhibitors of NSP2Pro chikungunya virus (CHIKV)
Source: NCGC
External Id: APP-Toga-CHIKV-nsp2-p

Name: Inhibition of mTORC1 in human CLL cells assessed as reduction in c-Myc expression at ...
Source: ChEMBL
Target: Target of rapamycin complex subunit LST8
External Id: CHEMBL5720107

Name: Thermal Shift Assay. Domain: start/stop: E122-S403
Source: ChEMBL
Target: Aurora kinase A
External Id: CHEMBL5067447

Name: Inhibition of mTORC1 in human NCI-H929 cells assessed as reduction in c-Myc expressio...
Source: ChEMBL
Target: Target of rapamycin complex subunit LST8
External Id: CHEMBL5720109

Name: Inhibition of mTORC1 in human SLL cells assessed as reduction in c-Myc expression at ...
Source: ChEMBL
Target: Target of rapamycin complex subunit LST8
External Id: CHEMBL5720108

Name: Inhibition of mTORC1 in human CLL cells assessed as reduction in 4E-BP1 phosphorylati...
Source: ChEMBL
Target: Target of rapamycin complex subunit LST8
External Id: CHEMBL5720111

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(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

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Shanghai Nianxing Industrial Co., Ltd
China
Product Name: TGR-1202
Price: Check
Purity: 98.0%
Delivery: 10 Day
Contact: Yang
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Price: $166/10mM*1mLinDMSO

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tgr-1202

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The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.