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TGR-1202 R-enantiomer

Names

[ CAS No. ]:
1532533-69-9

[ Name ]:
TGR-1202 R-enantiomer

[Synonym ]:
2-{(1R)-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
4H-1-Benzopyran-4-one, 2-[(1R)-1-[4-amino-3-[3-fluoro-4-(1-methylethoxy)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-6-fluoro-3-(3-fluorophenyl)-

Biological Activity

[Description]:

Umbralisib R-enantiomer (TGR-1202 R-enantiomer) is a PI3Kδ inhibitor, which is the less active enantiomer of TGR-1202.

[Related Catalog]:

Research Areas >> Cancer

[Target]

PI3Kδ


[In Vitro]

Umbralisib R-enantiomer (TGR-1202 R-enantiomer) (Formula A) exhibits a 50% inhibitory concentration (IC50) with respect to the δ type PI3-kinase that is at least 20-fold lower than the inhibitor's IC50 with respect to the rest of the other PI3K isoforms (i.e., a, β, and γ)[1].

[References]

[1]. Michael Weiss, et al. Combination of anti-cd20 antibody and pi3 kinase selective inhibitor. WO2014071125A1.


[Related Small Molecules]

3-Methyladenine | LY294002 | Wortmannin | Alpelisib (BYL719) | BKM120 | Eganelisib(IPI-549) | BAY 80-6946 (Copanlisib) | Idelalisib (CAL-101) | Dactolisib (BEZ235) | Quercetin | SAR-405 | GDC-0941 | 740 Y-P | LY3023414 | 1,3-Dicaffeoylquinic acid

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
737.4±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C31H24F3N5O3

[ Molecular Weight ]:
571.549

[ Flash Point ]:
399.8±32.9 °C

[ Exact Mass ]:
571.183105

[ LogP ]:
6.66

[ Vapour Pressure ]:
0.0±2.4 mmHg at 25°C

[ Index of Refraction ]:
1.666

[ Storage condition ]:
2-8℃

Related Compounds