Fimepinostat
Based on 15 publication(s) in Google Scholar
Fimepinostat (CUDC-907) potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes with an IC50 of 19/54/39 nM and 1.7/5.0/1.8/2.8 nM for PI3Kα/PI3Kβ/PI3Kδ and HDAC1/HDAC2/HDAC3/HDAC10 , respectively.
For research use only. We do not sell to patients.
- Purity: 99.95%
- CAS No.: 1339928-25-4
- Formula: C23H24N8O4S
- Molecular Weight:508.55
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Fimepinostat
More- J Clin Invest. 2025 Jun 2;135(11):e187490. [Abstract]
- J Exp Clin Cancer Res. 2020 Oct 17;39(1):219. [Abstract]
- Acta Pharmacol Sin. 2019 May;40(5):677-688 [Abstract]
- NPJ Precis Oncol. 2025 Nov 21;9(1):373. [Abstract]
- EMBO J. 2024 Nov;43(21):4954-4983. [Abstract]
- J Clin Endocrinol Metab. 2021 Jan 1;106(1):e232-e246. [Abstract]
- Chem Biol Interact. 2025 Sep 9:421:111735. [Abstract]
- Sci Rep. 2022 Apr 12;12(1):6090. [Abstract]
- Cancers (Basel). 2022 Feb 20;14(4):1067. [Abstract]
- Cancer Res Commun. 2023 Aug 17;3(8):1580-1593. [Abstract]
- ACS Med Chem Lett. 2015 Jun 22;6(8):948-52. [Abstract]
- Int J Parasitol Drugs Drug Resist. 2026 May 17;31:100649.
- bioRxiv. 2025 Aug 25.
- Research Square Print. 2023 Mar 9.
- SSRN. 2022 Nov 21.
-
Cell Proliferation/Viability Assay
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WB
-
In Vivo Efficacy Study
-
IF
-
IHC
Biological Activity
|
PI3Kα 19 nM (IC50) |
PI3Kδ 39 nM (IC50) |
PI3Kβ 54 nM (IC50) |
PI3Kγ 311 nM (IC50) |
HDAC1 1.7 nM (IC50) |
HDAC3 1.8 nM (IC50) |
HDAC10 2.8 nM (IC50) |
HDAC2 5 nM (IC50) |
HDAC11 5.4 nM (IC50) |
HDAC6 27 nM (IC50) |
HDAC8 191 nM (IC50) |
HDAC4 409 nM (IC50) |
HDAC7 426 nM (IC50) |
HDAC9 554 nM (IC50) |
HDAC5 674 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | EC50 |
126.25 nM
Compound: CUDC-907
|
Inhibition of HDAC1/2/3 in human A2780S cells assessed as histone H3 acetylation incubated for 6 hrs by cytoblot assay
Inhibition of HDAC1/2/3 in human A2780S cells assessed as histone H3 acetylation incubated for 6 hrs by cytoblot assay
|
[PMID: 27186676] |
| A2780 | EC50 |
221.75 nM
Compound: CUDC-907
|
Inhibition of HDAC6 in human A2780S cells assessed as tubulin acetylation incubated for 6 hrs by cytoblot assay
Inhibition of HDAC6 in human A2780S cells assessed as tubulin acetylation incubated for 6 hrs by cytoblot assay
|
[PMID: 27186676] |
| A2780 | IC50 |
6.15 nM
Compound: CUDC-907
|
Cytotoxicity against human A2780S cells assessed as growth inhibition after 24 hrs by MTT assay
Cytotoxicity against human A2780S cells assessed as growth inhibition after 24 hrs by MTT assay
|
[PMID: 27186676] |
| ASPC1 | IC50 |
2 nM
Compound: 32; CUDC-907
|
Antiproliferative activity against human ASPC1 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human ASPC1 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 37875056] |
| Bel-7402 | IC50 |
0.013 μM
Compound: 10; CUDC-907
|
Antiproliferative activity against human Bel7402 cells after 96 hrs by MTT assay
Antiproliferative activity against human Bel7402 cells after 96 hrs by MTT assay
|
[PMID: 31117517] |
| BXPC-3 | IC50 |
2 nM
Compound: 32; CUDC-907
|
Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 37875056] |
| Capan-2 | IC50 |
0.007 μM
Compound: 10; CUDC-907
|
Antiproliferative activity against human Capan2 cells after 96 hrs by MTT assay
Antiproliferative activity against human Capan2 cells after 96 hrs by MTT assay
|
[PMID: 31117517] |
| CFPAC-1 | IC50 |
2 nM
Compound: 32; CUDC-907
|
Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 37875056] |
| CWR22R | IC50 |
2 nM
Compound: 32; CUDC-907
|
Antiproliferative activity against human 22Rv1 cells assessed as inhibition of cell growth measured after 72 hrs by SRB assay
Antiproliferative activity against human 22Rv1 cells assessed as inhibition of cell growth measured after 72 hrs by SRB assay
|
[PMID: 37875056] |
| DU-145 | IC50 |
0.56 μM
Compound: 10; CUDC-907
|
Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay
Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay
|
[PMID: 31117517] |
| DU-145 | IC50 |
2 nM
Compound: 32; CUDC-907
|
Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth measured after 72 hrs by SRB assay
Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth measured after 72 hrs by SRB assay
|
[PMID: 37875056] |
| HCT-116 | IC50 |
0.005 μM
Compound: 10; CUDC-907
|
Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay
Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay
|
[PMID: 31117517] |
| HCT-116 | IC50 |
7.34 nM
Compound: CUDC-907
|
Cytotoxicity against human HCT116 cells assessed as growth inhibition after 24 hrs by MTT assay
Cytotoxicity against human HCT116 cells assessed as growth inhibition after 24 hrs by MTT assay
|
[PMID: 27186676] |
| HCT-8 | IC50 |
0.005 μM
Compound: 10; CUDC-907
|
Antiproliferative activity against human HCT8 cells after 96 hrs by MTT assay
Antiproliferative activity against human HCT8 cells after 96 hrs by MTT assay
|
[PMID: 31117517] |
| HeLa | IC50 |
6.8 nM
Compound: CUDC-907
|
Inhibition of HDAC in human HeLa cell nuclear extract using Ac-Leu-Gly-Lys (Ac)-AMC as substrate after 30 mins by fluorescence assay
Inhibition of HDAC in human HeLa cell nuclear extract using Ac-Leu-Gly-Lys (Ac)-AMC as substrate after 30 mins by fluorescence assay
|
[PMID: 27186676] |
| HepG2 | IC50 |
0.015 μM
Compound: 10; CUDC-907
|
Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay
|
[PMID: 31117517] |
| HGC-27 | IC50 |
0.041 μM
Compound: 10; CUDC-907
|
Antiproliferative activity against human HGC27 cells after 96 hrs by MTT assay
Antiproliferative activity against human HGC27 cells after 96 hrs by MTT assay
|
[PMID: 31117517] |
| HPAC | IC50 |
2 nM
Compound: 32; CUDC-907
|
Antiproliferative activity against human HPAC cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human HPAC cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 37875056] |
| Huh-7 | IC50 |
0.56 μM
Compound: 10; CUDC-907
|
Antiproliferative activity against human HuH7 cells after 96 hrs by MTT assay
Antiproliferative activity against human HuH7 cells after 96 hrs by MTT assay
|
[PMID: 31117517] |
| K562 | IC50 |
0.28 μM
Compound: 10; CUDC-907
|
Antiproliferative activity against human K562 cells after 96 hrs by MTT assay
Antiproliferative activity against human K562 cells after 96 hrs by MTT assay
|
[PMID: 31117517] |
| KYSE-30 | IC50 |
2 nM
Compound: 32; CUDC-907
|
Antiproliferative activity against human KYSE-30 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against human KYSE-30 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
|
[PMID: 37875056] |
| KYSE-450 | IC50 |
2 nM
Compound: 32; CUDC-907
|
Antiproliferative activity against human KYSE-450 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against human KYSE-450 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
|
[PMID: 37875056] |
| KYSE-510 | IC50 |
2 nM
Compound: 32; CUDC-907
|
Antiproliferative activity against human KYSE-510 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against human KYSE-510 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
|
[PMID: 37875056] |
| LAPC4 | IC50 |
2 nM
Compound: 32; CUDC-907
|
Antiproliferative activity against human LAPC4 cells assessed as inhibition of cell growth measured after 72 hrs by SRB assay
Antiproliferative activity against human LAPC4 cells assessed as inhibition of cell growth measured after 72 hrs by SRB assay
|
[PMID: 37875056] |
| LNCaP | IC50 |
2 nM
Compound: 32; CUDC-907
|
Antiproliferative activity against human LNCaP cells assessed as inhibition of cell growth measured after 72 hrs by SRB assay
Antiproliferative activity against human LNCaP cells assessed as inhibition of cell growth measured after 72 hrs by SRB assay
|
[PMID: 37875056] |
| LNCaP C4-2 | IC50 |
2 nM
Compound: 32; CUDC-907
|
Antiproliferative activity against human C4-2 cells assessed as inhibition of cell growth measured after 72 hrs by SRB assay
Antiproliferative activity against human C4-2 cells assessed as inhibition of cell growth measured after 72 hrs by SRB assay
|
[PMID: 37875056] |
| LNCaP C4-2B | IC50 |
2 nM
Compound: 32; CUDC-907
|
Antiproliferative activity against human LNCaP C4-2B cells assessed as inhibition of cell growth measured after 72 hrs by SRB assay
Antiproliferative activity against human LNCaP C4-2B cells assessed as inhibition of cell growth measured after 72 hrs by SRB assay
|
[PMID: 37875056] |
| MCF7 | IC50 |
0.041 μM
Compound: 10; CUDC-907
|
Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay
|
[PMID: 31117517] |
| MDA-MB-453 | IC50 |
0.009 μM
Compound: 10; CUDC-907
|
Antiproliferative activity against human MDA-MB-453 cells after 96 hrs by MTT assay
Antiproliferative activity against human MDA-MB-453 cells after 96 hrs by MTT assay
|
[PMID: 31117517] |
| MIA PaCa-2 | IC50 |
2 nM
Compound: 32; CUDC-907
|
Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 37875056] |
| MV4-11 | IC50 |
0.43 nM
Compound: CUDC-907
|
Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 24 hrs by MTT assay
Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 24 hrs by MTT assay
|
[PMID: 27186676] |
| NCI-H1299 | IC50 |
0.025 μM
Compound: 10; CUDC-907
|
Antiproliferative activity against human NCI-H1299 cells after 96 hrs by MTT assay
Antiproliferative activity against human NCI-H1299 cells after 96 hrs by MTT assay
|
[PMID: 31117517] |
| NCI-H460 | IC50 |
0.15 μM
Compound: 10; CUDC-907
|
Antiproliferative activity against human NCI-H460 cells after 96 hrs by MTT assay
Antiproliferative activity against human NCI-H460 cells after 96 hrs by MTT assay
|
[PMID: 31117517] |
| PANC-1 | IC50 |
2 nM
Compound: 32; CUDC-907
|
Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 37875056] |
| PC-3 | IC50 |
2 nM
Compound: 32; CUDC-907
|
Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth measured after 72 hrs by SRB assay
Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth measured after 72 hrs by SRB assay
|
[PMID: 37875056] |
| Sf9 | IC50 |
0.36 nM
Compound: 10; CUDC-907
|
Inhibition of recombinant C-terminal His/FLAG-tagged HDAC1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr
Inhibition of recombinant C-terminal His/FLAG-tagged HDAC1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr
|
[PMID: 31117517] |
| Sf9 | IC50 |
1.4 nM
Compound: 10; CUDC-907
|
Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr
Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr
|
[PMID: 31117517] |
| Sf9 | IC50 |
1.6 nM
Compound: 10; CUDC-907
|
Inhibition of recombinant human full length HDAC2 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr
Inhibition of recombinant human full length HDAC2 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr
|
[PMID: 31117517] |
| Sf9 | IC50 |
1.8 nM
Compound: CUDC-907
|
Inhibition of full length C-terminal His-tagged human recombinant HDAC3/NCOR2 (395 to 489 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substr
Inhibition of full length C-terminal His-tagged human recombinant HDAC3/NCOR2 (395 to 489 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substr
|
[PMID: 27186676] |
| Sf9 | IC50 |
132 nM
Compound: 10; CUDC-907
|
Inhibition of recombinant human full length HDAC11 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr
Inhibition of recombinant human full length HDAC11 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr
|
[PMID: 31117517] |
| Sf9 | IC50 |
19 nM
Compound: 24; CUDC-907
|
Inhibition of recombinant human full-length N-terminal GST-tagged p110alpha/untagged full-length p85alpha expressed in baculovirus infected Sf9 cells using PIP2 as substrate by ADP-glo luminescence assay
Inhibition of recombinant human full-length N-terminal GST-tagged p110alpha/untagged full-length p85alpha expressed in baculovirus infected Sf9 cells using PIP2 as substrate by ADP-glo luminescence assay
|
[PMID: 30418766] |
| Sf9 | IC50 |
19 nM
Compound: CUDC-907
|
Inhibition of full length recombinant human N-terminal GST-tagged p110 alpha/untagged p85 alpha expressed in baculovirus infected insect Sf9 cells using PI:3PS as substrate incubated for 60 mins by ADP-Glo luminescence assay
Inhibition of full length recombinant human N-terminal GST-tagged p110 alpha/untagged p85 alpha expressed in baculovirus infected insect Sf9 cells using PI:3PS as substrate incubated for 60 mins by ADP-Glo luminescence assay
|
[PMID: 27186676] |
| Sf9 | IC50 |
191 nM
Compound: CUDC-907
|
Inhibition of full length C-terminal His-tagged human recombinant HDAC8 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after
Inhibition of full length C-terminal His-tagged human recombinant HDAC8 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after
|
[PMID: 27186676] |
| Sf9 | IC50 |
2.8 nM
Compound: CUDC-907
|
Inhibition of human recombinant HDAC10 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay
Inhibition of human recombinant HDAC10 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay
|
[PMID: 27186676] |
| Sf9 | IC50 |
27 nM
Compound: CUDC-907
|
Inhibition of full length human recombinant HDAC6 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a
Inhibition of full length human recombinant HDAC6 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a
|
[PMID: 27186676] |
| Sf9 | IC50 |
39 nM
Compound: 24; CUDC-907
|
Inhibition of recombinant human full-length N-terminal GST-tagged p110delta/untagged full-length p85alpha expressed in baculovirus infected Sf9 cells using PIP2 as substrate by ADP-glo luminescence assay
Inhibition of recombinant human full-length N-terminal GST-tagged p110delta/untagged full-length p85alpha expressed in baculovirus infected Sf9 cells using PIP2 as substrate by ADP-glo luminescence assay
|
[PMID: 30418766] |
| Sf9 | IC50 |
39 nM
Compound: CUDC-907
|
Inhibition of N-terminal His6-tagged recombinant full-length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected insect Sf9 cells incubated for 2 hrs by kinase-glo assay
Inhibition of N-terminal His6-tagged recombinant full-length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected insect Sf9 cells incubated for 2 hrs by kinase-glo assay
|
[PMID: 27186676] |
| Sf9 | IC50 |
409 nM
Compound: CUDC-907
|
Inhibition of N-terminal GST/C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrat
Inhibition of N-terminal GST/C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrat
|
[PMID: 27186676] |
| Sf9 | IC50 |
426 nM
Compound: CUDC-907
|
Inhibition of N-terminal GST-tagged human recombinant HDAC7 (518 to end residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measu
Inhibition of N-terminal GST-tagged human recombinant HDAC7 (518 to end residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measu
|
[PMID: 27186676] |
| Sf9 | IC50 |
445 nM
Compound: 10; CUDC-907
|
Inhibition of recombinant human full length HDAC4 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr
Inhibition of recombinant human full length HDAC4 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr
|
[PMID: 31117517] |
| Sf9 | IC50 |
5 nM
Compound: CUDC-907
|
Inhibition of full length human recombinant HDAC2 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a
Inhibition of full length human recombinant HDAC2 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a
|
[PMID: 27186676] |
| Sf9 | IC50 |
5.4 nM
Compound: CUDC-907
|
Inhibition of full length human recombinant HDAC11 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence
Inhibition of full length human recombinant HDAC11 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence
|
[PMID: 27186676] |
| Sf9 | IC50 |
54 nM
Compound: 24; CUDC-907
|
Inhibition of recombinant human full-length N-terminal GST-tagged p110beta/untagged full-length p85alpha expressed in baculovirus infected Sf9 cells using PIP2 as substrate by ADP-glo luminescence assay
Inhibition of recombinant human full-length N-terminal GST-tagged p110beta/untagged full-length p85alpha expressed in baculovirus infected Sf9 cells using PIP2 as substrate by ADP-glo luminescence assay
|
[PMID: 30418766] |
| Sf9 | IC50 |
54 nM
Compound: CUDC-907
|
Inhibition of recombinant human p110beta expressed in baculovirus infected insect Sf9 cells incubated for 1 hr by ADP-gloreagen assay
Inhibition of recombinant human p110beta expressed in baculovirus infected insect Sf9 cells incubated for 1 hr by ADP-gloreagen assay
|
[PMID: 27186676] |
| Sf9 | IC50 |
554 nM
Compound: CUDC-907
|
Inhibition of C-terminal His-tagged human recombinant HDAC9 (604 to 1066 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition meas
Inhibition of C-terminal His-tagged human recombinant HDAC9 (604 to 1066 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition meas
|
[PMID: 27186676] |
| Sf9 | IC50 |
674 nM
Compound: CUDC-907
|
Inhibition of human recombinant HDAC5 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay
Inhibition of human recombinant HDAC5 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay
|
[PMID: 27186676] |
| SW1990 | IC50 |
0.18 μM
Compound: 10; CUDC-907
|
Antiproliferative activity against human SW1990 cells after 96 hrs by MTT assay
Antiproliferative activity against human SW1990 cells after 96 hrs by MTT assay
|
[PMID: 31117517] |
| U-87MG ATCC | IC50 |
0.007 μM
Compound: 10; CUDC-907
|
Antiproliferative activity against human U87 cells after 96 hrs by MTT assay
Antiproliferative activity against human U87 cells after 96 hrs by MTT assay
|
[PMID: 31117517] |
Fimepinostat is a potent pan-inhibitor of HDAC classes I and II enzymes and observed that its potency against class I HDACs is similar to that of LBH589 and greater than that of SAHA. Fimepinostat is also a potent inhibitor of class I PI3K kinases with an IC50 of 19, 54, and 39 nM for PI3Kα, PI3Kβ, and PI3Kδ, respectively. Fimepinostat markedly induces p21 protein in H460, a non-small cell lung cancer (NSCLC) cell line. Fimepinostat causes the reduction of both p-STAT3 (Y-705) and p-SRC in RPMI-8226 multiple myeloma cells and reduces both phosphorylated and total protein levels of MET and EGFR as well as HER2 and HER3 in H1975 NSCLC cells and BT-474 breast cancer cells, respectively. Fimepinostat induces caspase-3 and -7 activation in HCT-116 colon cancer cells in a dose-dependent manner. Fimepinostat potently inhibits the growth of cancer cells derived from both hematologic and solid tumors. Fimepinostat potently inhibits the proliferation of cells expressing either mutant or wild-type PI3K[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 1339928-25-4
-
Appearance Solid
-
Molecular Weight 508.55
-
Formula C23H24N8O4S
-
Color White to light yellow
-
SMILES
O=C(C1=CN=C(N(CC2=CC3=NC(C4=CC=C(OC)N=C4)=NC(N5CCOCC5)=C3S2)C)N=C1)NO
-
Synonyms
CUDC-907
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (15)
-
Journal Impact Factor
-
Most Recent
-
J Clin Invest
2025 Jun 2;135(11):e187490. PMID: 40454483
Fimepinostat purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2025 Jun 2;135(11):e187490. [Abstract]
The indicated cell lines were treated with Fimepinostat , and cell viability was measured by CellTiter-Glo assays. IC50 values are shown.
Fimepinostat purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2025 Jun 2;135(11):e187490. [Abstract]
The indicated cell lines were treated with 5 nM Fimepinostat, 2 nM Romidepsin, or 500 nM Entinostat for 48 hours. The indicated proteins were measured by Western blot. Histone H3 serves as loading control.
Fimepinostat purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2025 Jun 2;135(11):e187490. [Abstract]
NSG mice were implanted with DNPC BCaP-1 PDXs and treated with vehicle, Fimepinostat (75 mg/kg orally, 5 times per week), or Romidepsin (1.5 mg/kg intraperitoneally, 2 times per week). Tumor volume (top) and mouse body weight (bottom) are shown.
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J Exp Clin Cancer Res
The dual HDAC-PI3K inhibitor CUDC-907 displays single-agent activity and synergizes with PARP inhibitor olaparib in small cell lung cancer. [Abstract]2020 Oct 17;39(1):219. PMID: 33069237
Fimepinostat purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2020 Oct 17;39(1):219. [Abstract]
DNA damage detected by comet assay in SCLC cells upon treatment with 10 nM CUDC-907 or 10 μM olaparib alone and in combination for 48 h.
Fimepinostat purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2020 Oct 17;39(1):219. [Abstract]
Representative immunohistochemistry images of Ki67, cleaved-caspase3 (CC3), c-MYC, Rad51, and Ku80 on PDX tumors treated with CUDC-907 (75 mg/kg) and olaparib alone or in combination.
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Acta Pharmacol Sin
CUDC-907 displays potent antitumor activity against human pancreatic adenocarcinoma in vitro and in vivo through inhibition of HDAC6 to downregulate c-Myc expression. [Abstract]2019 May;40(5):677-688 PMID: 30224636
Fimepinostat purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2019 May;40(5):677-688 [Abstract]
Aspc-1 and Capan-1 cells are collected for Western blotting with the indicated antibodies after treatment with CUDC-907 for 48 h.
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NPJ Precis Oncol
Integrative profiling strategies to guide personalized therapy in mantle cell lymphoma: a pilot study. [Abstract]2025 Nov 21;9(1):373. PMID: 41272086 -
EMBO J
Acetylation of TIR domains in the TLR4-Mal-MyD88 complex regulates immune responses in sepsis. [Abstract]2024 Nov;43(21):4954-4983. PMID: 39294473 -
J Clin Endocrinol Metab
2021 Jan 1;106(1):e232-e246. PMID: 33000123 -
Chem Biol Interact
CUDC-907 exerts an inhibitory effect on non-small cell lung cancer associated with induction of mitotic catastrophe and downregulation of YAP/TAZ signaling. [Abstract]2025 Sep 9:421:111735. PMID: 40935272 -
Sci Rep
QSAR analysis on a large and diverse set of potent phosphoinositide 3-kinase gamma (PI3Kγ) inhibitors using MLR and ANN methods. [Abstract]2022 Apr 12;12(1):6090. PMID: 35414065 -
Cancers (Basel)
2022 Feb 20;14(4):1067. PMID: 35205815 -
Cancer Res Commun
Activator Protein-1 (AP-1) Signaling Inhibits the Growth of Ewing Sarcoma Cells in Response to DNA Replication Stress. [Abstract]2023 Aug 17;3(8):1580-1593. PMID: 37599787 -
ACS Med Chem Lett
High-Throughput Screening of Patient-Derived Cultures Reveals Potential for Precision Medicine in Glioblastoma. [Abstract]2015 Jun 22;6(8):948-52. PMID: 26288699 -
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Solvent & Solubility
DMSO : 43.75 mg/mL (86.03 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
DMF : 5 mg/mL (9.83 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.09 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.09 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
The activities of classes I and II HDACs are measured using the Color-de-Lys assay system. The activity of PI3K is measured using the ADP-Glo luminescent kinase assay. Recombinant PI3K protein, a complex of N-terminal GST-tagged recombinant full-length human p110 and untagged recombinant full-length human p85, is coexpressed in a baculovirus-infected Sf9 cell expression system[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Human cancer cell lines are plated at densities of 5,000 to 10,000 per well in 96-well flat-bottomed plates with the recommended culture medium. The cells are then incubated with compounds (e.g.,Fimepinostat) at various concentrations for 72 hours in culture medium supplemented with 0.5% (v/v) FBS. Growth inhibition is assessed by assay of cellular ATP content using the Perkin-Elmer ATPlite kit[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Six- to 8-week-old female athymic (nude nu/nu CD-1) or severe combined immunodeficient (SCID) mice obtained from Charles River Laboratories are injected subcutaneously with 3 to 20×106 cells in a medium suspension of 100 to 200 μL into the right hind flank region. Varying doses of Fimepinostat, standard anticancer agents, or vehicle are administered orally or via tail vein injection as indicated.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMF / DMSO | 1 mM | 1.9664 mL | 9.8319 mL | 19.6638 mL | 49.1594 mL |
| 5 mM | 0.3933 mL | 1.9664 mL | 3.9328 mL | 9.8319 mL | |
| DMSO | 10 mM | 0.1966 mL | 0.9832 mL | 1.9664 mL | 4.9159 mL |
| 15 mM | 0.1311 mL | 0.6555 mL | 1.3109 mL | 3.2773 mL | |
| 20 mM | 0.0983 mL | 0.4916 mL | 0.9832 mL | 2.4580 mL | |
| 25 mM | 0.0787 mL | 0.3933 mL | 0.7866 mL | 1.9664 mL | |
| 30 mM | 0.0655 mL | 0.3277 mL | 0.6555 mL | 1.6386 mL | |
| 40 mM | 0.0492 mL | 0.2458 mL | 0.4916 mL | 1.2290 mL | |
| 50 mM | 0.0393 mL | 0.1966 mL | 0.3933 mL | 0.9832 mL | |
| 60 mM | 0.0328 mL | 0.1639 mL | 0.3277 mL | 0.8193 mL | |
| 80 mM | 0.0246 mL | 0.1229 mL | 0.2458 mL | 0.6145 mL |