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Fimepinostat (CUDC-907)

Fimepinostat (CUDC-907)

ArtNr	S2759-10
Hersteller	Selleckchem
CAS-Nr.	1339928-25-4
Menge	10 mg
Quantity options	10 mg 10 mM/1 mL 200 mg 5 mg 50 mg
Kategorie	Oncology Neuroscience Aging & Neurological Disorders Neural Epigenetics Inhibitors & Compound Libraries Small Molecules By Organ Skin Cancer Heart & Blood Cancer Lymphatic System Cancer
Typ	Inhibitors
Specific against	other
Smiles	CN(CC1=CC2=C(S1)C(=NC(=N2)C3=CN=C(C=C3)OC)N4CCOCC4)C5=NC=C(C=N5)C(=O)NO
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	1339928-25-4'
Similar products	PI3K/HDAC
Lieferbar
Manufacturer - Targets	HDAC3, HDAC2, HDAC1, PI3K
Storage Conditions	2 years -80 in solvent
Molecular Weight	508, 55
Administration	Administered via p.o.
Animal Models	NHL and MM models in mice
Dosages	100 mg/kg
IC50	19 nM, 19 nM, 19 nM, 19 nM, 19 nM, 19 nM
In vitro	PI3K/HDAC Inhibitor I inhibits other PI3K isoforms such as PI3Kbeta, PI3Kgamma, PI3Kdelta, PI3K H1047R and PI3K E545K with IC50 of 54 nM, 311 nM, 39 nM, 73 nM and 62 nM, respectively. Moreover, PI3K/HDAC Inhibitor I also prevents HDAC subtypes HDAC8, HDAC6 and HDAC11 with IC50 of 191 nM, 27 nM and 5.4 nM, respectively. [1] In addition, PI3K/HDAC Inhibitor I suppresses other types of HDAC enzymatic activity with lower potency. PI3K/HDAC Inhibitor I inhibits the growth of a series of B cell lymphoma such as Granta 519, DOHH2, RL, Pfeiffer, SuDHL4, Daudi and Raji with IC50 of 7 nM, 1 nM, 2 nM, 4 nM, 3 nM, 15 nM and 9 nM, respectively. PI3K/HDAC Inhibitor I also blocks the proliferation of Myeloma including RPMI8226, OPM-2 and ARH77 with IC50 of 2 nM, 1 nM and 5 nM, respectively. PI3K/HDAC Inhibitor I displays greater anti-tumor activity in multiple myeloma and B cell lymphoma. [1]
In vivo	PI3K/HDAC Inhibitor I has a long half-life in murine tumors. PI3K/HDAC Inhibitor I induces apoptosis and inhibits cancer cell proliferation in xenograft tumors. [1] In efficacy studies in NHL and MM models, PI3K/HDAC Inhibitor I is more efficacious than either a single-agent PI3K or HDAC inhibitor reference compound or a combination of the two agents given at maximally tolerated doses (MTD). Furthermore, PI3K/HDAC Inhibitor I is more efficacious than the PI3Kdelta-selective inhibitor CAL-101 when dosed at MTD doses. [1]
Solubility (25C)	DMSO 102 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. CUDC-907 induces cell cycle arrest and apoptosis in breast cancer cells. Phase 1.
Chemical Name	N-hydroxy-2-(((2-(6-methoxypyridin-3-yl)-4-morpholinothieno[3, 2-d]pyrimidin-6-yl)methyl)(methyl)amino)pyrimidine-5-carboxamide

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S2759-10-datasheet.pdf

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