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PI3K/HDAC Inhibitor

PI3K/HDAC Inhibitor structure

CAS No:
1339928-25-4
Formula:
C23H24N8O4S
Chemical Name:
PI3K/HDAC Inhibitor
Synonyms:
PI3K/HDAC Inhibitor;CUDC-907;CUDC-907 /CUDC907;N-Hydroxy-2-[[[2-(6-methoxypyridin-3-yl)-4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-6-yl]methyl](methyl)amino]pyrimidine-5-carboxamide;N-hydroxy-2-(((2-(6-methoxypyridin-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)(methyl)amino)pyrimidine-5-carboxamide;N-Hydroxy-2-[[[2-(6-methoxypyridin-3-yl)-4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-6-yl]methyl](methyl)amino]pyrimidine-5-carboxamideCUDC-907;N-hydroxy-2-(((2-(6-methoxypyridin-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)(methyl)amino)pyrimidine-5-carboxamidemethanesulfonate;EOS-62197
Categories:
Biochemical Engineering > Inhibitors

Description

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.

CUDC-907 has been used in trials studying the treatment of Lymphoma, Solid Tumors, BREAST CANCER, Multiple Myeloma, and NUT Midline Carcinoma, among others.|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, fimepinostat 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.

PI3K/HDAC Inhibitor Basic Attributes

Molecular Weight：

508.55286

Exact Mass：

508.164124

UNII：

3S9RX35S5X

DSSTox ID：

DTXSID90712307

NCI Thesaurus Code：

C104008

Characteristics

PSA：

167

XLogP3：

1.3

Density：

1.445±0.06 g/cm3(Predicted)

Refractive Index：

1.696

Drug Information

MeSH Entry Terms：

CUDC-907

PI3K/HDAC Inhibitor Use and Manufacturing

CUDC-907 is a dual PI3K and HDAC inhibitor. Studies have shown CUDC-907 is able to enhance antitumor activity when combined with standard of care agents in multiple myeloma and B cell lymphoma xenograft models.

Computed Properties

Molecular Weight:508.6
XLogP3:1.3
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:12
Rotatable Bond Count:7
Exact Mass:508.16412245
Monoisotopic Mass:508.16412245
Topological Polar Surface Area:167
Heavy Atom Count:36
Complexity:726
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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CAS No.: 1339928-25-4

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CAS No.: 1339928-25-4

Grade: Industrial Grade

Content: 99%

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