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Chemical Structure| 2376146-48-2 Chemical Structure| 2376146-48-2

Structure of Azenosertib
CAS No.: 2376146-48-2

Chemical Structure| 2376146-48-2

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Azenosertib (ZN-c3) is an orally effective selective inhibitor of Wee1 (IC50=3.9 nM). Azenosertib has antitumor activity.

Synonyms: Zn-C3

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Product Details of Azenosertib

CAS No. :2376146-48-2
Formula : C29H34N8O2
M.W : 526.63
SMILES Code : C=CCN1N(C2=CC=C(CC[C@]3(O)CC)C3=N2)C4=NC(NC5=CC=C(N6CCN(CC6)C)C=C5)=NC=C4C1=O
Synonyms :
Zn-C3
MDL No. :MFCD34567336

Safety of Azenosertib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
H460 cells 1 μM 72 h WEE1 inhibitors had minimal effect on cell viability Cell Rep Med. 2024 Jun 18;5(6):101578
H358 cells 1 μM 72 h WEE1 inhibitors significantly inhibited cell viability Cell Rep Med. 2024 Jun 18;5(6):101578
OV90 1.3 nM to 10 μM 72 h To evaluate the growth inhibition effect of Azenosertib on OV90 cells, results showed that Azenosertib treatment resulted in partial growth inhibition or cytostatic effect. NPJ Precis Oncol. 2025 Jan 4;9(1):3
OVCAR4 1.3 nM to 10 μM 72 h To evaluate the growth inhibition effect of Azenosertib on OVCAR4 cells, results showed that Azenosertib treatment resulted in significant cytotoxicity. NPJ Precis Oncol. 2025 Jan 4;9(1):3
OVCAR3 1.3 nM to 10 μM 72 h To evaluate the growth inhibition effect of Azenosertib on OVCAR3 cells, results showed that Azenosertib treatment resulted in significant cytotoxicity. NPJ Precis Oncol. 2025 Jan 4;9(1):3
NCI-H2122 250 nM 24 h Evaluate the synergistic effect of Azenosertib combined with KRASG12C inhibitors, showing significant increases in DNA damage and apoptosis markers (γH2AX and c-Casp-3/7). Cancer Res Commun. 2025 Feb 1;5(2):240-252

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD/SCID mice OVCAR3 xenograft model Oral 80 mg/kg Once daily for 28 days To evaluate the anti-tumor activity of Azenosertib in the OVCAR3 xenograft model, results showed that a dose of 80 mg/kg resulted in 88% tumor growth inhibition. NPJ Precis Oncol. 2025 Jan 4;9(1):3
Mice H358 xenograft model Oral 60 mg/kg 5 days per week for 3–5 weeks ZN-c3 monotherapy and combination with sotorasib effectively suppressed tumor growth Cell Rep Med. 2024 Jun 18;5(6):101578
NOD/SCID mice NCI-H2122 CDX model Oral 60 mg/kg Once daily for 25 days Evaluate the antitumor activity of Azenosertib alone and in combination with sotorasib, showing complete tumor regression (104% TGI) with combination therapy. Cancer Res Commun. 2025 Feb 1;5(2):240-252

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT06369155 Uterine Serous Carcinoma|Uteri... More >>ne Carcinoma|Uterine Cancer Less << PHASE2 NOT_YET_RECRUITING 2027-01-31 Brigham and Women's Hospital, ... More >>Boston, Massachusetts, 02215, United States|Dana-Farber Cancer Institute, Boston, Massachusetts, 02215, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.90mL

0.38mL

0.19mL

9.49mL

1.90mL

0.95mL

18.99mL

3.80mL

1.90mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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