Search Site
Related Products
MK-1775Wee1 kinase inhibtor,potent and ATP-competitive

MK-1775

Catalog No. A5755
Size Price Stock Qty
10mM (in 1mL DMSO) $100.00 In stock
Evaluation Sample $28.00 In stock
5mg $85.00 In stock
10mg $130.00 In stock
50mg $395.00 In stock
100mg $660.00 In stock

Tel: +1-832-696-8203

Email: sales@apexbt.com

Worldwide Distributors

Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

MK-1775

Related Biological Data

MK-1775

Related Biological Data

MK-1775

Related Biological Data

MK-1775

Biological Activity

Description MK-1775 is a potent and selective inhibitor of Wee1 with IC50 of 5.2 nM.
Targets Wee1          
IC50 5.2 nM          

MK-1775 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

MK-1775 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 955365-80-7 SDF Download SDF
Synonyms MK1775,MK 1775
Chemical Name 1-[6-(2-hydroxypropan-2-yl)pyridin-2-yl]-6-[4-(4-methylpiperazin-1-yl)anilino]-2-prop-2-enylpyrazolo[3,4-d]pyrimidin-3-one
Canonical SMILES CC(C)(C1=NC(=CC=C1)N2C3=NC(=NC=C3C(=O)N2CC=C)NC4=CC=C(C=C4)N5CCN(CC5)C)O
Formula C27H32N8O2 M.Wt 500.6
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

MK-1775 is a potent and selective small molecule inhibitor of Wee1 kinase, with an IC50 value of 5.2 nM in in vitro kinase assays. It functions as a Wee1 inhibitor in an ATP-competitive manner [1].

Previous research has shown that MK-1775 inhibited Wee1 activity and abrogated the DNA damage checkpoint usually in p53-deficient cells. It sensitized p53-inactivated tumor cells to various antitumor agents, including gemcitabine, carboplatin, cisplatin and radiation in both in vitro and in vivo settings. Moreover, only sequential treatment with the DNA-damaging agent followed by MK-1775 increased cytotoxic effects of these antitumor agents and enhanced cell death induction [1]. MK-1775 also inhibited Cdc2 Y15 phosphorylation in cells, but MK-1775 monotherapy did not induce tumor regression in some cases. Hence, a combination of DNA-damaging agents with MK-1775 is usually offered to produce dramatic antitumor activity [1]. A recent study demonstrated that heterogeneous distribution to brain tumors can limit the efficacy of MK-1775 combined with temozolomide in glioblastoma multiforme [2].

Meanwhile, MK-1775 also acts as a single antitumor agent for inducing apoptosis in sarcoma cells. The cytotoxic effect of MK-1775 on sarcoma cells seems to be independent of p53 status [3]. Another research showed that MK-1775 could also induce DNA damage without additional chemotherapy or radiation in S-phase cells. PKMYT1, a kinase functionally related to Wee1, might serve as an enrichment biomarker for MK-1775 sensitivity. Depletion of PKMYT1 decreases the EC(50) of MK-1775 by five-fold but has no effect on the sensitivity of other cytotoxic drugs. In addition, depletion of PKMYT1 promotes the DNA damage by MK-1775 [4].

References:
Hirai H, Iwasawa Y, Okada M et al.  Small-molecule inhibition of Wee1 kinase by MK-1775 selectively sensitizes p53-deficient tumor cells to DNA-damaging agents. Mol Cancer Ther. 2009 Nov;8(11):2992-3000.
Pokorny JL, Calligaris D, Gupta SK et al.  The Efficacy of the Wee1 Inhibitor MK-1775 Combined with Temozolomide Is Limited by Heterogeneous Distribution across the Blood-Brain Barrier in Glioblastoma. Clin Cancer Res. 2015 Apr 15;21(8):1916-24.
3.  Kreahling JM, Gemmer JY, Reed D et al. MK1775, a selective Wee1 inhibitor, shows single-agent antitumor activity against sarcoma cells. Mol Cancer Ther. 2012 Jan;11(1):174-82.
4.  Guertin AD, Li J, Liu Y et al. Preclinical evaluation of the WEE1 inhibitor MK-1775 as single-agent anticancer therapy. Mol Cancer Ther. 2013 Aug;12(8):1442-52.