Cat. No.: HY-13522

Fimepinostat

(Synonyms: CUDC-907)

15 Cited Publications

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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.

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Pureté: 99.95%
CAS No.: 1339928-25-4
Formule: C₂₃H₂₄N₈O₄S
Masse moléculaire:508.55

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Fimepinostat Chemical Structure

CAS No.: 1339928-25-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (15)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
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Activité biologique

Description

IC₅₀ & Target^[1]

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)

Voir tous les produits spécifiques à Isoform PI3K :

Voir tous les produits spécifiques à Isoform HDAC :

Cellular Effect

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]

In Vitro

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.

In Vivo

Oral administration of Fimepinostat inhibits growth of the Daudi cancer cell xenografts in a dose-dependent manner. Tumor stasis is observed at 100 mg/kg in this model without obvious toxicity. Importantly, in the same model, Fimepinostat achieves better efficacy than GDC-0941, SAHA, or a combination of these 2 compounds given at their maximal tolerated doses (MTD). Furthermore, Fimepinostat causes tumor regression or stasis after intravenous (50 mg/kg) or oral administration (100 mg/kg) in a xenograft tumor model of SU-DHL4 diffuse large B-cell lymphoma (DLBCL) and causes tumor stasis in KRAS-mutant A549 NSCLC cell xenografts^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1339928-25-4
Appearance Solid
Masse moléculaire 508.55
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (15)

All Cell Proliferation/Viability AssayIFWBIHCIn Vivo Efficacy Study

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Journal Impact Factor

J Clin Invest

PROX1 is an early driver of lineage plasticity in prostate cancer. [Abstract]

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.
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.
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.
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

Targeting Corticotroph HDAC and PI3-Kinase in Cushing Disease. [Abstract]

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)

Dual Targeting of PI3K and HDAC by CUDC-907 Inhibits Pediatric Neuroblastoma Growth. [Abstract]

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
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.

Solvant et solubilité

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9664 mL

9.8319 mL

19.6637 mL

5 mM

0.3933 mL

1.9664 mL

3.9328 mL

10 mM

0.1966 mL

0.9832 mL

1.9664 mL

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.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.08 mg/mL (4.09 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 10 mg/mL (19.66 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 30% SBE-β-CD in Saline

Solubility: 10 mg/mL (19.66 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protocole

Kinase Assay^[1]

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.

Cell Assay^[1]

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.

Animal Administration^[1]

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.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Qian C, et al. Cancer network disruption by a single molecule inhibitor targeting both histone deacetylase activity and phosphatidylinositol 3-kinase signaling. Clin Cancer Res. 2012 Aug 1;18(15):4104-13. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
DMF / DMSO	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

Keywords

Fimepinostat

15 Cited Publications

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Fimepinostat

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

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Cancer Stem Cells Compound Library

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Pain-Related Compound Library

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Publications Citing Use of MedChemExpress (MCE) Fimepinostat

Voir tous les produits spécifiques à Isoform PI3K

Voir tous les produits spécifiques à Isoform HDAC

Activité biologique

Chemical Information

Publications (15)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Fimepinostat Related Classifications

HY-13522 Related Classifications