Adavosertib (MK-1775), Wee1 checkpoint kinase inhibitor (TBI5462)

Description

Product Details

Formal Name: 1,2-Dihydro-1-[6-(1-hydroxy-1-methylethyl)-2-pyridinyl]-6-[[4-(4-methyl-1-piperazinyl)-phenyl]amino]-2-(2-propen-1-yl)-3H-pyrazolo[3,4-d]pyrimidin-3-one

Alternate Names: MK-1775; AZD 1775

Molecular Formula: C₂₇H₃₂N₈O₂

Formula Weight: 500.60

CAS Number: 955365-80-7

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (70 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

 

Applications

Wee1 checkpoint kinase inhibitor

 

Functions

Inhibits Wee1 tyrosine kinase (IC50 = 5.2 nM) thus preventing phosphorylation of CDC2 and abrogating the G₂ DNA damage checkpoint, sensitizing a variety of tumor cells to DNA damaging agents. Adavosertib also blocks Wee1 phosphorylation of E3 ubiquitin ligase SKP2 in human cells, ultimately preventing degradation of CDKs and further allowing cell cycle progression. Stimulates anti-tumor immunity and enhances sensitivity to immune checkpoint blockade by activating ERV and the dsRNA pathway. Potentiates sensitivity of tumors to PARP inhibitors.

 

Application Procedures

First dissolved in DMSO (70 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Additional information

SIZE (mg)	25 MG, 5 MG

TBI5462_Adavosertib (MK-1775)