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MedKoo Cat#: 465412 | Name: Azenosertib
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Azenosertib, also known as ZN-c3, is a highly selective Wee1 inhibitor (ICV50 = 3.8 nM) with balanced potency, ADME, and pharmacokinetic properties. ZN-c3 showed excellent in vivo efficacy. When ZN-c3 binds to Wee1, it disrupts the cell's reproduction cycle, which can make tumor cells more vulnerable to chemotherapy drugs and cause them to die.

Chemical Structure

Azenosertib
Azenosertib
CAS#2376146-48-2

Theoretical Analysis

MedKoo Cat#: 465412

Name: Azenosertib

CAS#: 2376146-48-2

Chemical Formula: C29H34N8O2

Exact Mass: 526.2805

Molecular Weight: 526.65

Elemental Analysis: C, 66.14; H, 6.51; N, 21.28; O, 6.08

Price and Availability

Size Price Availability Quantity
5mg USD 750.00 2 Weeks
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Related CAS #
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Synonym
ZN-c3; ZNc3; ZN c3; azenosertib;
IUPAC/Chemical Name
(R)-2-allyl-1-(7-ethyl-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-2-yl)-6-((4-(4-methylpiperazin-1-yl)phenyl)amino)-1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one
InChi Key
OXTSYWDBUVRXFF-GDLZYMKVSA-N
InChi Code
InChI=1S/C29H34N8O2/c1-4-14-36-27(38)23-19-30-28(31-21-7-9-22(10-8-21)35-17-15-34(3)16-18-35)33-26(23)37(36)24-11-6-20-12-13-29(39,5-2)25(20)32-24/h4,6-11,19,39H,1,5,12-18H2,2-3H3,(H,30,31,33)/t29-/m1/s1
SMILES Code
O=C1N(CC=C)N(C2=CC=C(CC[C@@]3(CC)O)C3=N2)C4=NC(NC5=CC=C(N6CCN(C)CC6)C=C5)=NC=C41
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Inhibition of Wee1 promotes both premature mitosis and a prolonged mitotic arrest leading to cell death in susceptible tumor cells, such as p53-deficient or mutated human cancers that lack the G1 checkpoint, upon treatment with DNA-damaging chemotherapeutic agents. Unlike normal cells, most p53-deficient or mutated human cancers lack the G1 checkpoint as p53 is the key regulator of the G1 checkpoint and these cells rely on the G2 checkpoint for DNA repair to damaged cells. Annulment of the G2 checkpoint may therefore make p53-deficient tumor cells more vulnerable to antineoplastic agents and enhance their cytotoxic effect. Overexpression of Wee1 occurs in several cancer types and high expression of Wee1 is associated with poor outcomes. Wee1 phosphorylates Cdc2 in the Cdc2/cyclin B (CDK1/cyclin B) complex which blocks progression from G2 into mitosis; it negatively regulates the G2 checkpoint by disallowing entry into mitosis in response to DNA damage.

Preparing Stock Solutions

The following data is based on the product molecular weight 526.65 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Huang PQ, Boren BC, Hegde SG, Liu H, Unni AK, Abraham S, Hopkins CD, Paliwal S, Samatar AA, Li J, Bunker KD. Discovery of ZN-c3, a Highly Potent and Selective Wee1 Inhibitor Undergoing Evaluation in Clinical Trials for the Treatment of Cancer. J Med Chem. 2021 Aug 23. doi: 10.1021/acs.jmedchem.1c01121. Epub ahead of print. PMID: 34423975. 2: Wu XN, Zhao HT, Li J, Schlangen M, Schwarz H. Highly regioselective hydride transfer, oxidative dehydrogenation, and hydrogen-atom abstraction in the thermal gas-phase chemistry of [Zn(OH)](+)/C3H8. Phys Chem Chem Phys. 2014 Dec 28;16(48):26617-23. doi: 10.1039/c4cp02139h. PMID: 25230924. 3: Jameson NM, Kim D, Lee C, Skrable B, Shea A, Guo X, Izadi H, Abed M, Harismendy O, Ma J, Kim DS, Lackner MR. The Selective WEE1 Inhibitor Azenosertib Shows Synergistic Antitumor Activity with KRASG12C Inhibitors in Preclinical Models. Cancer Res Commun. 2025 Feb 1;5(2):240-252. doi: 10.1158/2767-9764.CRC-24-0411. PMID: 39807828; PMCID: PMC11795354. 4: Kim D, Chung H, Liu W, Jeong K, Ozmen TY, Ozmen F, Rames MJ, Kim S, Guo X, Jameson N, de Jong PR, Yea S, Harford L, Li J, Mathews CA, Doroshow DB, Charles VJ, Kim D, Fischer K, Samatar AA, Jubb A, Bunker KD, Blackwell K, Simpkins F, Meric-Bernstam F, Mills GB, Harismendy O, Ma J, Lackner MR. Cyclin E1/CDK2 activation defines a key vulnerability to WEE1 kinase inhibition in gynecological cancers. NPJ Precis Oncol. 2025 Jan 4;9(1):3. doi: 10.1038/s41698-024-00787-4. PMID: 39755818; PMCID: PMC11700143. 5: Fukuda K, Takeuchi S, Arai S, Nanjo S, Sato S, Kotani H, Kita K, Nishiyama A, Sakaguchi H, Ohtsubo K, Yano S. Targeting WEE1 enhances the antitumor effect of KRAS-mutated non-small cell lung cancer harboring TP53 mutations. Cell Rep Med. 2024 Jun 18;5(6):101578. doi: 10.1016/j.xcrm.2024.101578. Epub 2024 May 21. PMID: 38776912; PMCID: PMC11228449.