Umbralisib

ChemicalBook > CAS DataBase List > Umbralisib

Product Name: 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
Formula Weight: 571.55
MOL File: 1532533-67-7.mol

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Umbralisib Property

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

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word: Warning

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N-Bromosuccinimide Price

TRC

Product number: R700975
Product name: RP5264
Packaging: 2.5mg
Price: $85
Updated: 2021/12/16

ChemScene

Product number: CS-5243
Product name: Umbralisib
Purity: 98.55%
Packaging: 5mg
Price: $120
Updated: 2021/12/16

ChemScene

Product number: CS-5243
Product name: Umbralisib
Purity: 98.55%
Packaging: 10mg
Price: $220
Updated: 2021/12/16

ChemScene

Product number: CS-5243
Product name: Umbralisib
Purity: 98.55%
Packaging: 25mg
Price: $440
Updated: 2021/12/16

ChemScene

Product number: CS-5243
Product name: Umbralisib
Purity: 98.55%
Packaging: 50mg
Price: $580
Updated: 2021/12/16

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Umbralisib Chemical Properties,Usage,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 %).

target

PI3Kδ, CK1ε

Umbralisib Preparation Products And Raw materials

Raw materials

Preparation Products

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1532533-67-7, UmbralisibRelated Search:

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