CUDC-907

貨號 Cat. No.: S2759
規格 Size: 5~200mg
品牌 Brand: Selleckchem

Description

CUDC-907

Catalog No.S2759

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. Phase 1.

Size

Price

Stock

Quantity

10mM/1mLIn DMSO	USD 693	In stock	0 1 2 3 4 5 6 7 8 9 10
5mg	USD 340	In stock	0 1 2 3 4 5 6 7 8 9 10
10mg	USD 466	In stock	0 1 2 3 4 5 6 7 8 9 10
50mg	USD 1348	In stock	0 1 2 3 4 5 6 7 8 9 10
200mg	USD 3112	In stock	0 1 2 3 4 5 6 7 8 9 10

Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

Biological Activity

Description	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. Phase 1.
Targets	PI3KÉ‘	HDAC1	HDAC2	HDAC3	HDAC10
IC50	19 nM	1.7 nM	5 nM	1.8 nM	2.8 nM ^[1]
In vitro	CUDC-907 inhibits other PI3K isoforms such as PI3Kβ, PI3Kγ, PI3Kδ, PI3KÉ‘H1047R and PI3KÉ‘E545K with IC50 of 54 nM, 311 nM, 39 nM, 73 nM and 62 nM, respectively. Moreover, CUDC-907 also prevents HDAC subtypes HDAC8, HDAC6 and HDAC11 with IC50 of 191 nM, 27 nM and 5.4 nM, respectively. ^[1] In addition, CUDC-907 suppresses other types of HDAC enzymatic activity with lower potency. CUDC-907 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. CUDC-907 also blocks the proliferation of Myeloma including RPMI8226, OPM-2 and ARH77 with IC50 of 2 nM, 1 nM and 5 nM, respectively. CUDC-907 displays greater anti-tumor activity in multiple myeloma and B cell lymphoma. ^[1]
In vivo	CUDC-907 has a long half-life in murine tumors. CUDC-907 induces apoptosis and inhibits cancer cell proliferation in xenograft tumors. ^[1] In efficacy studies in NHL and MM models, CUDC-907 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, CUDC-907 is more efficacious than the PI3Kδ-selective inhibitor CAL-101 when dosed at MTD doses. ^[1]
Features

Protocol(Only for Reference)

Animal Study: ^[1]

Animal Models	NHL and MM models in mice
Dosages	100 mg/kg
Administration	Administered via p.o.

References

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT01872260	Not yet recruiting	Breast Cancer	Novartis\|Novartis Pharmaceuticals	2013-07	Phase 1\|Phase 2
NCT01838577	Not yet recruiting	EGFR Mutation Positive Non Small Cell Lung Cancer	European Organisation for Research and Treatment of Cancer - EORTC	2013-09
NCT01870726	Not yet recruiting	Recurrent Glioblastoma	Novartis\|Novartis Pharmaceuticals	2013-09	Phase 1\|Phase 2
NCT01550380	Not yet recruiting	Endometrial Cancer	UniversityUtah\|Novartis	2013-12	Phase 2
NCT01723800	Not yet recruiting	Adenocarcinoma of the Lung\|Bronchoalveolar Cell Lung Cancer\|Large Cell Lung Cancer\|Recurrent Non-small Cell Lung Cancer\|Stage IV Non-small Cell Lung Cancer	City of Hope Medical Center\|National Cancer Institute (NCI)	2014-01	Phase 1

Chemical Information

Download CUDC-907 SDF

Molecular Weight (MW)	508.55
Formula	C₂₃H₂₄N₈O₄S
CAS No.	1339928-25-4

Storage	3 years -20â„ƒPowder
Storage	6 months-80â„ƒin DMSO
Syonnyms	N/A

Solubility (25°C) *	In vitro	DMSO	102 mg/mL (200 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	<1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.