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ChemicalBook > Product Catalog >Biochemical Engineering >Inhibitors >Umbralisib

Umbralisib

Umbralisib Structure
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
MOL File:
1532533-67-7.mol
MSDS File:
SDS
Modify Date:
2024/7/2 8:55:13
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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)
color White to off-white

SAFETY

Risk and Safety Statements

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

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.

brand name

Ukonig

General Description

Class: lipid kinase; Treatment: MZL, FL; Other name: TGR-1202; Elimination half-life = 91 h; Protein binding > 99.7%

Pharmacokinetics

Umbralisib has a prolonged half-life of 91 h, which enables once-daily dosing. However, the recommended dosage of 800 mg is the highest among all the PI3K inhibitors in use, presumably due to its limited oral bioavailability.

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

target

PI3Kδ, CK1ε

Umbralisib Preparation Products And Raw materials

Raw materials

1532533-34-8 1532533-36-0 1532533-31-5 3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine 2-(3-Fluoro-4-isopropoxyphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane
1300582-10-8 1532533-32-6 4-Bromo-2-fluorophenol 2-(4'-BROMO-2'-FLUOROPHENOXY)PROPANE 1-(5-Fluoro-2-hydroxyphenyl)-2-(3-fluorophenyl)ethanone
TGR-1202 (R-enantiomer) 3-Fluorophenylacetic acid 4-Fluoroanisole
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Preparation Products

Umbralisib Suppliers

Global( 75)Suppliers
Supplier Tel Country ProdList Advantage Inquiry
A.J Chemicals 91-9810153283 New Delhi, India 6124 58 Inquiry
BOC Sciences +1-631-485-4226 United States 19553 58 Inquiry
Wuhan Demeikai Biotechnology Co., Ltd +8618942921723 China 723 58 Inquiry
InvivoChem +1-708-310-1919 +1-13798911105 United States 6393 58 Inquiry
Nanjing Doge Biomedical Technology Co., Ltd +86-25-58227606 +86-15305155328 China 4128 58 Inquiry
TargetMol Chemicals Inc. +1-781-999-5354 United States 19973 58 Inquiry
Shanghai Huici Pharmaceutical Technology Co., LTD +8618917134367 China 133 58 Inquiry
Shanghai Huici Pharmaceutical Technology Co., LTD +8618917134367 China 133 58 Inquiry
Wuhan Topule Biopharmaceutical Co., Ltd +8618327326525 China 8474 58 Inquiry
LEAPCHEM CO., LTD. +86-852-30606658 China 43348 58 Inquiry
Supplier Advantage
A.J Chemicals 58
BOC Sciences 58
Wuhan Demeikai Biotechnology Co., Ltd 58
InvivoChem 58
Nanjing Doge Biomedical Technology Co., Ltd 58
TargetMol Chemicals Inc. 58
Shanghai Huici Pharmaceutical Technology Co., LTD 58
Shanghai Huici Pharmaceutical Technology Co., LTD 58
Wuhan Topule Biopharmaceutical Co., Ltd 58
LEAPCHEM CO., LTD. 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