Onvansertib fumarate | CAS# 1263293-37-3 | PLK1 inhibitor

MedKoo Cat#: 414438 | Name: Onvansertib fumarate

Description:

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

Onvansertib, also know as NMS-P937, PCM-075 and NMS1286937, is an oral Polo-like kinase 1 (PLK1) inhibitor, a key regulator of cell cycle progression and mitosis. It selectively inhibits PLK1 with a reported half-maximal inhibitory concentration (IC₅₀) of approximately 2 nM, while demonstrating significantly lower activity against other Polo-like kinases (PLK2 and PLK3). Onvansertib has shown potent anti-proliferative effects in various cancer cell lines, particularly in colorectal cancer, acute myeloid leukemia (AML), and prostate cancer models. It induces mitotic arrest, leading to apoptosis in tumor cells. Onvansertib has demonstrated synergistic effects when combined with chemotherapeutics such as irinotecan, 5-fluorouracil (5-FU), and decitabine, enhancing their efficacy in resistant cancers.

Chemical Structure

Onvansertib fumarate

CAS#1263293-37-3 (fumarate)

Theoretical Analysis

MedKoo Cat#: 414438

Name: Onvansertib fumarate

CAS#: 1263293-37-3 (fumarate)

Chemical Formula: C28H31F3N8O7

Exact Mass: 648.2268

Molecular Weight: 648.60

Elemental Analysis: C, 51.85; H, 4.82; F, 8.79; N, 17.28; O, 17.27

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

1034616-18-6 (free base) 1263293-37-3 (fumarate)

Synonym

Onvansertib fumarate; PMS-075H; PMS075H; PMS 075H; NMSP937 fumarate; NMS P937 fumarate; NMS-P937 fumarate

IUPAC/Chemical Name

1H-Pyrazolo(4,3-H)quinazoline-3-carboxamide, 4,5-dihydro-1-(2-hydroxyethyl)-8-((5-(4-methyl-1-piperazinyl)-2-(trifluoromethoxy)phenyl)amino)-, (2E)-2-butenedioate (1:1)

InChi Key

LUEMEFHVOJNLJG-WLHGVMLRSA-N

InChi Code

InChI=1S/C24H27F3N8O3.C4H4O4/c1-33-6-8-34(9-7-33)15-3-5-18(38-24(25,26)27)17(12-15)30-23-29-13-14-2-4-16-20(22(28)37)32-35(10-11-36)21(16)19(14)31-23;5-3(6)1-2-4(7)8/h3,5,12-13,36H,2,4,6-11H2,1H3,(H2,28,37)(H,29,30,31);1-2H,(H,5,6)(H,7,8)/b;2-1+

SMILES Code

O=C(C1=NN(CCO)C2=C1CCC3=CN=C(NC4=CC(N5CCN(C)CC5)=CC=C4OC(F)(F)F)N=C23)N.O=C(O)/C=C/C(O)=O

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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 648.60 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.

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: Zhang G, Pannucci A, Ivanov AA, Switchenko J, Sun SY, Sica GL, Liu Z, Huang Y, Schmitz JC, Owonikoko TK. Polo-like Kinase 1 Inhibitors Demonstrate In Vitro and In Vivo Efficacy in Preclinical Models of Small Cell Lung Cancer. Cancers (Basel). 2025 Jan 28;17(3):446. doi: 10.3390/cancers17030446. PMID: 39941812; PMCID: PMC11815996. 2: Petrella S, Colombo M, Marabese M, Grasselli C, Panfili A, Chiappa M, Sancisi V, Craparotta I, Barbera MC, Cassanmagnago GA, Bolis M, Damia G. Onvansertib and Navitoclax Combination as a New Therapeutic Option for Mucinous Ovarian Carcinoma. Int J Mol Sci. 2025 Jan 8;26(2):472. doi: 10.3390/ijms26020472. PMID: 39859203; PMCID: PMC11765470. 3: Kim DE, Oh HJ, Kim HJ, Kim YB, Kim ST, Yim H. Synergistic two-step inhibition approach using a combination of trametinib and onvansertib in KRAS and TP53-mutated colorectal adenocarcinoma. Biomed Pharmacother. 2025 Jan;182:117796. doi: 10.1016/j.biopha.2024.117796. Epub 2024 Dec 28. PMID: 39731938. 4: Erratum: Onvansertib in Combination With Chemotherapy and Bevacizumab in Second-Line Treatment of KRAS-Mutant Metastatic Colorectal Cancer: A Single-Arm, Phase II Trial. J Clin Oncol. 2025 Jan;43(1):113. doi: 10.1200/JCO-24-02458. Epub 2024 Nov 19. Erratum for: J Clin Oncol. 2025 Mar;43(7):840-851. doi: 10.1200/JCO-24-01266. PMID: 39561313. 5: Ahn DH, Ridinger M, Cannon TL, Mendelsohn L, Starr JS, Hubbard JM, Kasi A, Barzi A, Samuëlsz E, Karki A, Subramanian RA, Yemane D, Kim R, Wu CC, Croucher PJP, Smeal T, Kabbinavar FF, Lenz HJ. Onvansertib in Combination With Chemotherapy and Bevacizumab in Second-Line Treatment of KRAS-Mutant Metastatic Colorectal Cancer: A Single-Arm, Phase II Trial. J Clin Oncol. 2025 Mar;43(7):840-851. doi: 10.1200/JCO-24-01266. Epub 2024 Oct 30. Erratum in: J Clin Oncol. 2025 Jan;43(1):113. doi: 10.1200/JCO-24-02458. PMID: 39475591; PMCID: PMC11856007. 6: Sreekumar S, Montaudon E, Klein D, Gonzalez ME, Painsec P, Derrien H, Sourd L, Smeal T, Marangoni E, Ridinger M. PLK1 Inhibitor Onvansertib Enhances the Efficacy of Alpelisib in PIK3CA-Mutated HR-Positive Breast Cancer Resistant to Palbociclib and Endocrine Therapy: Preclinical Insights. Cancers (Basel). 2024 Sep 25;16(19):3259. doi: 10.3390/cancers16193259. PMID: 39409880; PMCID: PMC11476299. 7: Chiappa M, Decio A, Guarrera L, Mengoli I, Karki A, Yemane D, Ghilardi C, Scanziani E, Canesi S, Barbera MC, Craparotta I, Bolis M, Fruscio R, Grasselli C, Ceruti T, Zucchetti M, Patterson JC, Lu RA, Yaffe MB, Ridinger M, Damia G, Guffanti F. Onvansertib treatment overcomes olaparib resistance in high-grade ovarian carcinomas. Cell Death Dis. 2024 Jul 22;15(7):521. doi: 10.1038/s41419-024-06894-1. PMID: 39039067; PMCID: PMC11263393. 8: Nouri M, Varkaris A, Ridinger M, Dalrymple SL, Dennehy CM, Isaacs JT, Einstein DJ, Brennen WN, Balk SP. AKT Inhibition Sensitizes to Polo-Like Kinase 1 Inhibitor Onvansertib in Prostate Cancer. Mol Cancer Ther. 2024 Oct 1;23(10):1404-1417. doi: 10.1158/1535-7163.MCT-23-0933. PMID: 38894678; PMCID: PMC11444904. 9: Stebbing J, Bullock AJ. Polo-like Kinase 1 Inhibition in KRAS-Mutated Metastatic Colorectal Cancer. Clin Cancer Res. 2024 May 15;30(10):2005-2007. doi: 10.1158/1078-0432.CCR-24-0251. PMID: 38470499. 10: Ahn DH, Barzi A, Ridinger M, Samuëlsz E, Subramanian RA, Croucher PJP, Smeal T, Kabbinavar FF, Lenz HJ. Onvansertib in Combination with FOLFIRI and Bevacizumab in Second-Line Treatment of KRAS-Mutant Metastatic Colorectal Cancer: A Phase Ib Clinical Study. Clin Cancer Res. 2024 May 15;30(10):2039-2047. doi: 10.1158/1078-0432.CCR-23-3053. PMID: 38231047; PMCID: PMC11094418. 11: Croucher PJP, Ridinger M, Becker PS, Lin TL, Silberman SL, Wang ES, Zeidan AM. Spliceosome mutations are associated with clinical response in a phase 1b/2 study of the PLK1 inhibitor onvansertib in combination with decitabine in relapsed or refractory acute myeloid leukemia. Ann Hematol. 2023 Nov;102(11):3049-3059. doi: 10.1007/s00277-023-05442-9. Epub 2023 Sep 13. PMID: 37702821; PMCID: PMC10567832. 12: Ansari WA, Rab SO, Saquib M, Sarfraz A, Hussain MK, Akhtar MS, Ahmad I, Khan MF. Pentafuhalol-B, a Phlorotannin from Brown Algae, Strongly Inhibits the PLK-1 Overexpression in Cancer Cells as Revealed by Computational Analysis. Molecules. 2023 Aug 3;28(15):5853. doi: 10.3390/molecules28155853. PMID: 37570823; PMCID: PMC10421442. 13: Lu J, Lei H, Bai X, Wang W, Liu C, Yang Y, Zou F, Wang L, Wang Y, Du G, Wang X, Sun C, Yu L, Ma M, Ye L, Wang H, Tian J, Zhang J. Design, synthesis, and biological evaluation of novel molecules as potent inhibitors of PLK1. Bioorg Chem. 2023 Oct;139:106711. doi: 10.1016/j.bioorg.2023.106711. Epub 2023 Jul 13. PMID: 37473479. 14: Wang R, Hou Y, Geng G, Zhu X, Wang Z, Cai W, Ye J, Zhao S, Mi Y, Jiang J. Onvansertib inhibits the proliferation and improves the cisplatin-resistance of lung adenocarcinoma via β-catenin/c-Myc signaling pathway. Am J Cancer Res. 2023 Feb 15;13(2):623-637. PMID: 36895968; PMCID: PMC9989612. 15: Patterson JC, Varkaris A, Croucher PJP, Ridinger M, Dalrymple S, Nouri M, Xie F, Varmeh S, Jonas O, Whitman MA, Chen S, Rashed S, Makusha L, Luo J, Isaacs JT, Erlander MG, Einstein DJ, Balk SP, Yaffe MB. Plk1 Inhibitors and Abiraterone Synergistically Disrupt Mitosis and Kill Cancer Cells of Disparate Origin Independently of Androgen Receptor Signaling. Cancer Res. 2023 Jan 18;83(2):219-238. doi: 10.1158/0008-5472.CAN-22-1533. PMID: 36413141; PMCID: PMC9852064. 16: Affatato R, Chiappa M, Guffanti F, Ricci F, Formenti L, Fruscio R, Jaconi M, Ridinger M, Erlander M, Damia G. Onvansertib and paclitaxel combined in platinum-resistant ovarian carcinomas. Ther Adv Med Oncol. 2022 May 31;14:17588359221095064. doi: 10.1177/17588359221095064. PMID: 35665077; PMCID: PMC9160919. 17: Su S, Chhabra G, Singh CK, Ndiaye MA, Ahmad N. PLK1 inhibition-based combination therapies for cancer management. Transl Oncol. 2022 Feb;16:101332. doi: 10.1016/j.tranon.2021.101332. Epub 2021 Dec 29. PMID: 34973570; PMCID: PMC8728518. 18: Hagege A, Ambrosetti D, Boyer J, Bozec A, Doyen J, Chamorey E, He X, Bourget I, Rousset J, Saada E, Rastoin O, Parola J, Luciano F, Cao Y, Pagès G, Dufies M. The Polo-like kinase 1 inhibitor onvansertib represents a relevant treatment for head and neck squamous cell carcinoma resistant to cisplatin and radiotherapy. Theranostics. 2021 Sep 21;11(19):9571-9586. doi: 10.7150/thno.61711. PMID: 34646387; PMCID: PMC8490521. 19: Wang D, Veo B, Pierce A, Fosmire S, Madhavan K, Balakrishnan I, Donson A, Alimova I, Sullivan KD, Joshi M, Erlander M, Ridinger M, Foreman NK, Venkataraman S, Vibhakar R. A novel PLK1 inhibitor onvansertib effectively sensitizes MYC-driven medulloblastoma to radiotherapy. Neuro Oncol. 2022 Mar 12;24(3):414-426. doi: 10.1093/neuonc/noab207. PMID: 34477871; PMCID: PMC8917408. 20: Bewersdorf JP, Zeidan AM. Polo-like kinase inhibition as a therapeutic target in acute myeloid leukemia. Oncotarget. 2021 Jun 22;12(13):1314-1317. doi: 10.18632/oncotarget.27919. PMID: 34194628; PMCID: PMC8238245.