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Umbralisib

CAS No.
1532533-67-7
Chemical Name:
Umbralisib
Synonyms
CS-2443;TGR1205;RP-5264;TGR-1202;Umbralisib;RP-5264 TGR-1202;RP5264;UMBRALISIB;TGR-1202(Umbralisib);Umbralisib (TGR-1202);RP5264; TGR1202; TGR 1202; RP-5264; RP 5264
CBNumber:
CB62716383
Molecular Formula:
C31H24F3N5O3
Molecular Weight:
571.55
MDL Number:
MFCD28386165
MOL File:
1532533-67-7.mol
MSDS File:
SDS
Last updated:2023-06-08 09:03:02

Umbralisib Properties

Boiling point 737.4±60.0 °C(Predicted)
Density 1.43±0.1 g/cm3(Predicted)
storage temp. Store at -20°C
solubility DMF: 1 mg/ml; DMSO: 1 mg/ml
form solid
pka 3.79±0.30(Predicted)
FDA UNII 38073MQB2A

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictogramsGHS hazard pictograms
GHS07,GHS09
Signal word  Warning
NFPA 704
0
2 0

Umbralisib price

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
TRC R700975 RP5264 1532533-67-7 2.5mg $85 2021-12-16 Buy
ChemScene CS-5243 Umbralisib 98.55% 1532533-67-7 5mg $120 2021-12-16 Buy
ChemScene CS-5243 Umbralisib 98.55% 1532533-67-7 10mg $220 2021-12-16 Buy
ChemScene CS-5243 Umbralisib 98.55% 1532533-67-7 25mg $440 2021-12-16 Buy
ChemScene CS-5243 Umbralisib 98.55% 1532533-67-7 50mg $580 2021-12-16 Buy
Product number Packaging Price Buy
R700975 2.5mg $85 Buy
CS-5243 5mg $120 Buy
CS-5243 10mg $220 Buy
CS-5243 25mg $440 Buy
CS-5243 50mg $580 Buy

Umbralisib Chemical Properties,Uses,Production

Description

Umbralisib (TGR-1202) tosylate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib tosylate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib tosylate can be used for haematological malignancies reseach. 

Uses

RP 5264 is a novel PI3K inhibitor that enhances Brentuximab Vedotin-induced lymphoma cell death.

Synthesis

The synthesis of Umbralisib is as follows:
To a solution of intermediate 13 (0.134 g, 0.494 mmol) in THF (2.0 ml), intermediate 5 (0.150 g, 0.494 mmol) and triphenylphosphine (0.194 g, 0.741 mml) were added and stirred at RT for 5 min. Diisopropylazodicarboxylate ( 0.15 ml, 0.749 mmol) was added heated to 45°C. After 2h, the reaction mixture was quenched with with water and extracted with ethyl acetate. The organic layer was dried over sodium sulphate and concentrated under reduced pressure. The crude product was purified by column chromatography with ethyl acetate : petroleum ether to afford Umbralisib as an off-white solid (0.049 g, 20 %).
synthesis of Umbralisib.png

2105-94-4
1532533-67-7
Synthesis of Umbralisib from 4-Bromo-2-fluorophenol

Umbralisib Suppliers

Global( 75)Suppliers
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BOC Sciences
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Wuhan Topule Biopharmaceutical Co., Ltd
+8618327326525 masar@topule.com China 8474 58
TGR-1202 RP-5264 RP-5264 TGR-1202 TGR1205 Umbralisib Umbralisib (TGR-1202) 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)- (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 RP5264;UMBRALISIB CS-2443 RP5264; TGR1202; TGR 1202; RP-5264; RP 5264 TGR-1202(Umbralisib) inhibit,RP-5264,lymphocytic leukemia,lymphoma,CLL T cells,Inhibitor,Umbralisib,haematological malignancies,cancer,orally active,PI3K,RP 5264,Phosphoinositide 3-kinase,Casein Kinase 1532533-67-7