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.
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Name | Azenosertib |
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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 |
Synonyms | ZN-c3; ZNc3; ZN c3; azenosertib; |
Molecular Formula | C29H34N8O2 |
Molecular Weight | 526.63 |
Smile | 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 |
InChiKey | OXTSYWDBUVRXFF-GDLZYMKVSA-N |
InChi | 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 |
CAS Number | 2376146-48-2 |
Related CAS |
Packaging | Price | Availability | Purity | Shipping Time |
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Formulation | Off-white solid |
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Purity | 98% Min. |
Storage | Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years). |
Solubility | Soluble in DMSO |
Handling | |
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. |
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Mechanism | |
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Clinical study |
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.