Fimepinostat
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MedKoo CAT#: 205924

CAS#: 1339928-25-4 (free base)

Description: CUDC-907, also known as fimepinostat, is an orally bioavailable inhibitor of both phosphoinositide 3-kinase (PI3K) class I and pan histone deacetylase (HDAC) enzymes, with potential antineoplastic activity. Upon oral administration, CUDC-907 inhibits the activity of both PI3K class I isoforms and HDAC, thereby preventing the activation of the PI3K-AKT-mTOR signal transduction pathway that is often overactivated in many cancer cell types. This may prevent growth of PI3K and/or HDAC-expressing tumor cells. CUDC-907 shows an increased inhibition of tumor cell growth and induction of apoptosis when compared to inhibitors that target either PI3K or HDAC.


Chemical Structure

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Fimepinostat
CAS# 1339928-25-4 (free base)

Theoretical Analysis

MedKoo Cat#: 205924
Name: Fimepinostat
CAS#: 1339928-25-4 (free base)
Chemical Formula: C23H24N8O4S
Exact Mass: 508.16
Molecular Weight: 508.550
Elemental Analysis: C, 54.32; H, 4.76; N, 22.03; O, 12.58; S, 6.31

Price and Availability

Size Price Availability Quantity
5mg USD 250 2 weeks
10mg USD 450 2 weeks
50mg USD 950 2 weeks
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Related CAS #: 1401998-36-4 (mesylate)   1339928-25-4 (free base)  

Synonym: CUDC907; CUDC 907; CUDC-907; fimepinostat;

IUPAC/Chemical Name: N-hydroxy-2-(((2-(6-methoxypyridin-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)(methyl)amino)pyrimidine-5-carboxamide

InChi Key: JOWXJLIFIIOYMS-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H24N8O4S/c1-30(23-25-11-15(12-26-23)22(32)29-33)13-16-9-17-19(36-16)21(31-5-7-35-8-6-31)28-20(27-17)14-3-4-18(34-2)24-10-14/h3-4,9-12,33H,5-8,13H2,1-2H3,(H,29,32)

SMILES Code: O=C(C1=CN=C(N(CC2=CC3=NC(C4=CC=C(OC)N=C4)=NC(N5CCOCC5)=C3S2)C)N=C1)NO

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: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

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:         

Biological target:
In vitro activity:
In vivo activity:

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
Soluble in DMSO, not in water 0.0 100.00

Preparing Stock Solutions

The following data is based on the product molecular weight 508.55 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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Gunst JD, Kjær K, Olesen R, Rasmussen TA, Østergaard L, Denton PW, Søgaard OS, Tolstrup M. Fimepinostat, a novel dual inhibitor of HDAC and PI3K, effectively reverses HIV-1 latency ex vivo without T cell activation. J Virus Erad. 2019 Sep 18;5(3):133-137. PMID: 31700655; PMCID: PMC6816120.


2: Landsburg DJ, Barta SK, Ramchandren R, Batlevi C, Iyer S, Kelly K, Micallef IN, Smith SM, Stevens DA, Alvarez M, Califano A, Shen Y, Bosker G, Parker J, Soikes R, Martinez E, von Roemeling R, Martell RE, Oki Y. Fimepinostat (CUDC-907) in patients with relapsed/refractory diffuse large B cell and high- grade B-cell lymphoma: report of a phase 2 trial and exploratory biomarker analyses. Br J Haematol. 2021 Oct;195(2):201-209. doi: 10.1111/bjh.17730. Epub 2021 Aug 2. PMID: 34341990.


3: Liao W, Yang W, Xu J, Yan Z, Pan M, Xu X, Zhou S, Zhu Y, Lan J, Zeng M, Han X, Li S, Li Y, Liang K, Gao Y, Peng Q. Therapeutic Potential of CUDC-907 (Fimepinostat) for Hepatocarcinoma Treatment Revealed by Tumor Spheroids-Based Drug Screening. Front Pharmacol. 2021 Oct 29;12:658197. doi: 10.3389/fphar.2021.658197. PMID: 34776939; PMCID: PMC8585736.


4: Pedot G, Marques JG, Ambühl PP, Wachtel M, Kasper S, Ngo QA, Niggli FK, Schäfer BW. Inhibition of HDACs reduces Ewing sarcoma tumor growth through EWS- FLI1 protein destabilization. Neoplasia. 2022 May;27:100784. doi: 10.1016/j.neo.2022.100784. Epub 2022 Mar 30. Retraction in: Neoplasia. 2023 Oct;44:100916. Erratum in: Neoplasia. 2022 Sep;31:100805. PMID: 35366465; PMCID: PMC8971315.


5: Chen J, Guanizo AC, Jakasekara WSN, Inampudi C, Luong Q, Garama DJ, Alamgeer M, Thakur N, DeVeer M, Ganju V, Watkins DN, Cain JE, Gough DJ. MYC drives platinum resistant SCLC that is overcome by the dual PI3K-HDAC inhibitor fimepinostat. J Exp Clin Cancer Res. 2023 Apr 26;42(1):100. doi: 10.1186/s13046-023-02678-1. PMID: 37098540; PMCID: PMC10131464.


6: Padalino G, Coghlan A, Pagliuca G, Forde-Thomas JE, Berriman M, Hoffmann KF. Using ChEMBL to Complement Schistosome Drug Discovery. Pharmaceutics. 2023 Apr 28;15(5):1359. doi: 10.3390/pharmaceutics15051359. PMID: 37242601; PMCID: PMC10220823.


7: Pan Y, Hou H, Zhou B, Gao J, Gao F. Hydroxamic acid hybrids: Histone deacetylase inhibitors with anticancer therapeutic potency. Eur J Med Chem. 2023 Dec 15;262:115879. doi: 10.1016/j.ejmech.2023.115879. Epub 2023 Oct 18. PMID: 37875056.


8: Zhang A, Lau NA, Wong A, Brown LG, Coleman IM, De Sarkar N, Li D, DeLucia DC, Labrecque MP, Nguyen HM, Conner JL, Dumpit RF, True LD, Lin DW, Corey E, Alumkal JJ, Nelson PS, Morrissey C, Lee JK. Concurrent Targeting of HDAC and PI3K to Overcome Phenotypic Heterogeneity of Castration-resistant and Neuroendocrine Prostate Cancers. Cancer Res Commun. 2023 Nov 20;3(11):2358-2374. doi: 10.1158/2767-9764.CRC-23-0250. PMID: 37823778; PMCID: PMC10658857.


9: Rice CA, Colon BL, Chen E, Hull MV, Kyle DE. Discovery of repurposing drug candidates for the treatment of diseases caused by pathogenic free-living amoebae. PLoS Negl Trop Dis. 2020 Sep 24;14(9):e0008353. doi: 10.1371/journal.pntd.0008353. PMID: 32970675; PMCID: PMC7546510.


10: Paxson AI, Chang LH, Gard JMC, Harryman WL, Nelson CS, Salmon SB, Marr KD, Wachsmuth LM, Ramanathan A, Ran J, Kapoor A, Marugan JJ, Henderson MJ, Sanchez TW, Cress AE. Phenotype plasticity and altered sensitivity to chemotherapeutic agents in aggressive prostate cancer cells. Front Cell Dev Biol. 2023 Nov 16;11:1285372. doi: 10.3389/fcell.2023.1285372. PMID: 38046670; PMCID: PMC10690371.


11: Huegel J, Dinh CT, Martinelli M, Bracho O, Rosario R, Hardin H, Estivill M, Griswold A, Gultekin S, Liu XZ, Fernandez-Valle C. CUDC907, a dual phosphoinositide-3 kinase/histone deacetylase inhibitor, promotes apoptosis of NF2 Schwannoma cells. Oncotarget. 2022 Jul 19;13:890-904. doi: 10.18632/oncotarget.28254. PMID: 35875610; PMCID: PMC9295707.


12: Chilamakuri R, Agarwal S. Dual Targeting of PI3K and HDAC by CUDC-907 Inhibits Pediatric Neuroblastoma Growth. Cancers (Basel). 2022 Feb 20;14(4):1067. doi: 10.3390/cancers14041067. PMID: 35205815; PMCID: PMC8870466.