Adavosertib | Wee1 kinase inhibitor

CAS:
955365-80-7
Catalog Number:
10-4823
Activity:
Wee1 kinase inhibitor
Chemical Names:
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 Name:
MK-1775; AZD1775
Molecular Weight:
500.61
Molecular Formula:
C27H32N8O2
Solubility:
Soluble in DMSO (70 mg/ml)
Physical Properties:
Yellow solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$45.00
25 mg$155.00

Adavosertib (955365-80-7) 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.1 Adavosertib also blocks Wee1 phosphorylation of E3 ubiquitin ligase SKP2 in human cells, ultimately preventing degradation of CDKs and further allowing cell cycle progression.2 Stimulates anti-tumor immunity and enhances sensitivity to immune checkpoint blockade by activating ERV and the dsRNA pathway.3 Potentiates sensitivity of tumors to PARP inhibitors.4

References/Citations:

  1. Hirai et al. (2009) Small-molecule inhibition of Wee1 kinase by MK-1775 selectively sensitizes p53-deficient tumor cells to DNA-damaging agents; Cancer Ther. 8 2992
  2. Pan et al. (2021) A novel WEE1 pathway for replication stress responses; Plants 7 209
  3. Guo et al. (2022) WEE1 inhibition induces anti-tumor immunity by activating ERV and the dsRNA pathway; Exp. Med. 219 e20210789
  4. Seo et al. (2021) Inhibition of WEE1 Potentiates Sensitivity to PARP Inhibitor in Biliary Tract Cancer; Cancer Res. Treat. Epub ahead of print
CAS:
955365-80-7
Catalog Number:
10-4823
Activity:
Wee1 kinase inhibitor
Chemical Names:
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 Name:
MK-1775; AZD1775
Molecular Weight:
500.61
Molecular Formula:
C27H32N8O2
Solubility:
Soluble in DMSO (70 mg/ml)
Physical Properties:
Yellow solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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