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MK-1775

HY-10993

(AZD-1775; AZD1775; AZD 1775)

MK-1775

MK-1775 Chemical Structure

MK-1775 is a potent and selective Wee1 inhibitor with IC50 of 5.2 nM; hinders G2 DNA damage checkpoint.

Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO $97 In-stock
5 mg $88 In-stock
10 mg $132 In-stock
50 mg $396 In-stock
100 mg $660 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €95 In-stock
5 mg €86 In-stock
10 mg €129 In-stock
50 mg €388 In-stock
100 mg €647 In-stock
200 mg Get quote
500 mg Get quote

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Product name: MK-1775
Cat. No.: HY-10993

MK-1775 Data Sheet

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    Purity: 99.30%

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Biological Activity of MK-1775

MK-1775 is a potent and selective Wee1 inhibitor with IC50 of 5.2 nM; hinders G2 DNA damage checkpoint.
IC50 Value: 5.2 nM
Target: Wee1
in vitro: MK-1775 inhibits Wee1 kinase in an ATP-competitive manner. Compared to Wee1, MK-1775 displays 2- to 3-fold less potency against Yes with IC50 of 14 nM, 10-fold less potency against seven other kinases with >80% inhibition at 1 μM, and >100-fold selectivity over human Myt 1, another kinase that inhibits cyclin-dependent kinase 1 (CDC2) by phosphorylation at an alternative site (Thr14). By abrogating the DNA damage checkpoint via blockade of Wee1 activity in WiDr cells bearing mutated p53, MK-1775 treatment inhibits the basal phosphorylation of CDC2 at Tyr15 (CDC2Y15) with EC50 of 49 nM, and suppresses gemcitabine-, carboplatin- or cisplatin-induced phosphorylation of CDC2 and cell cycle arrest in a dose-dependent manner, with EC50 of 82 nM and 81 nM, 180 nM and 163 nM, as well as 159 nM and 160 nM, respectively. MK-1775 treatment alone at 30-100 nM has no significant antiproliferative effect in WiDr and H1299 cells, whereas MK-1775 at 300 nM, sufficient to inhibit Wee1 by >80%, displays moderate but significant antiproliferative effects by 34.1% in WiDr cells and 28.4% in H1299 cells.
in vivo: MK-1775 treatment alone at ~20 mg/kg displays minimal antitumor effects against WiDr xenografts in rats with T/C of 69% at day 3. Antitumor efficacy by MK-1775 alone in the nude rat HeLa-luc and TOV21G-shp53 xenograft models models is also moderate.

Chemical Information

M.Wt 500.6 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C27H32N8O2
CAS No 955365-80-7
Solvent & Solubility

DMSO ≥98mg/mL Water <1.2mg/mL Ethanol ≥4.6mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 1.9976 mL 9.9880 mL 19.9760 mL
5 mM 0.3995 mL 1.9976 mL 3.9952 mL
10 mM 0.1998 mL 0.9988 mL 1.9976 mL

Clinical Information of MK-1775

Product Name Sponsor Only Condition Start Date End Date Phase Last Change Date
MK-1775 The University Health Network Metastatic head and neck cancer 30-SEP-13 31-MAR-16 Phase 2 12-SEP-13
Merck & Co Inc Ovary tumor 31-JUL-11 28-FEB-15 Phase 2 17-OCT-13
Merck & Co Inc Uterine cervix tumor 31-MAY-10 30-JUN-11 Phase 2 27-JUN-11
The University Health Network Squamous cell carcinoma 30-SEP-13 31-MAR-16 Phase 2 12-SEP-13
National Cancer Institute Advanced solid tumor 31-MAR-13 31-MAR-17 Phase 2 29-OCT-13
Netherlands Cancer Institute Ovary tumor 31-JUL-10 30-SEP-13 Phase 2 13-SEP-12

References on MK-1775

Inhibitor Kit