CUDC-907 --- PI3K/HDAC dual inhibitor

CUDC-907 is a potent inhibitor of class I PI3K kinases with an IC50 of 19 nM, 54 nM, 311 nM and 39 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ. It also potently inhibits HDAC1, HDAC2, HDAC3, HDAC6, HDAC10 and HDAC11 with IC50 of 1.7 nM, 5 nM, 1.8 nM, 27 nM, 2.8 nM and 5.4 nM respectively. Through its simultaneous HDAC inhibitory activity, CUDC-907 durably inhibits the PI3K-AKT-mTOR pathway and compensatory signaling molecules such as RAF, MEK, MAPK, and STAT-3, as well as upstream receptor tyrosine kinases. CUDC-907 induces apoptosis and G2–M cell-cycle arrest in cancer cells and effectively inhibits more than 50 different cancer cells’ growth. It may potentially evade drug resistance in cancer cells. CUDC-907 also inhibits targets and tumor growth in xenograft tumor models. Currently CUDC-907 is in phase I clinical trials for patients with solid tumors or lymphoma.

Product information

CAS Number: 1339928-25-4

Molecular Weight: 508.55

Formula: C23H24N8O4S

Synonym:

CUDC 907

CUDC907

fimepinostat

Related CAS Number:

1401998-36-4 (CUDC-907 mesylate)

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

Smiles: CN(CC1=CC2=NC(=NC(=C2S1)N1CCOCC1)C1=CN=C(C=C1)OC)C1N=CC(=CN=1)C(=O)NO

InChiKey: JOWXJLIFIIOYMS-UHFFFAOYSA-N

InChi: 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)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

CUDC-907 was used at 0.1-1 µM final concentration in vitro and in cellular assays.

In Vivo:

CUDC-907 was orally dosed to mice at 100 mg/kg or intravenously dosed at 50 mg/kg once per day in the xenograft tumor model of SU-DHL4 (DLBCL) and A549 (NSCLC).

References:

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

Products are for research use only. Not for human use.

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