CUDC-907 (PI3K/HDAC InhibitorI)|CAS 1339928-25-4|DC Chemicals

Cas No.:	1339928-25-4
Chemical Name:	Fimepinostat
Synonyms:	CUDC907,CUDC 907 (PI3K/HDAC InhibitorI)
SMILES:	O=C(C1=CN=C(N(CC2=CC3=NC(C4=CC=C(OC)N=C4)=NC(N5CCOCC5)=C3S2)C)N=C1)NO
Formula:	C₂₃H₂₄N₈O₄S
M.Wt:	508.55

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.
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, Vorinostat, 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].
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 panobinostat and greater than that of vorinostat. 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].

Cat. No.	Product name	Field of application
DC70802	SS-208	SS-208 (SS208) is a novel potent, selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 of 12 nM, >100-fold selectivity over HDAC1/4/5/7/8/9/11.SS-208 has minimal effects on the viability of murine SM1 melanoma cells in vitro, significantly reduced in vivo tumor growth in a murine SM1 syngeneic melanoma mouse model.
DC3110	CUDC-907 (PI3K/HDAC InhibitorI)	CUDC-907 (PI3K/HDAC Inhibitor I) is a dual PI3K and HDAC inhibitor for PI3Kɑ, HDAC1, HDAC2, HDAC3 and HDAC10 with IC50 of 19 nM, 1.7 nM, 5 nM, 1.8 nM and 2.8 nM, respectively.
DC8252	Vorinostat (SAHA)	Vorinostat (SAHA) is an HDAC1/3 inhibitor with IC50 of ~10 nM.
DC8663	UF010	UF010 is a potent and selective HADC inhibitor with IC50 ~0.06 μM, 0.1 μM, 0.5 μM and 1.5 μM for HDACs 3, 2, 1 and 8, respectively. It has > 6-fold selectivity over other HDACs.
DC6303	Tubastatin A HCl	Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold).
DC6304	Tubastatin A	Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold).
DC5178	Tubacin (BML-GR362)	Tubacin is a selective inhibitor of HDAC6 via inhibition of the second deacetylase domain (DD2).
DC8134	Trichostatin A (TSA)	Trichostatin A (TSA) is a selective and potent HDAC inhibitor with IC50 of ~1.8 nM; HDAC8 is the only known member of the HDAC-family that is not affected by TSA.
DC7716	TMP269	TMP269 is a novel and selective class IIa histone deacetylase inhibitor with IC50s of 126/80/36/9 nM for HDAC 4/5/7/9, respectively; 20-400 fold selectivity over class1 HDACs.
DC10210	TMP195	TMP195 is the most potent and selective class IIa HDAC inhibitor.