Varlitinib

貨號 Cat. No.: S2755
規格 Size: 5~200mg
品牌 Brand: Selleckchem

Description

Varlitinib

Catalog No.S2755

4 Reviews 1 Product Citations

ARRY334543 is a selective and potent ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively. Phase 2.

Size

Price

Stock

Quantity

10mM/1mLIn DMSO	USD 630	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	ARRY334543 is a selective and potent ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively. Phase 2.
Targets	ErbB2	ErbB1
IC50	2 nM	7 nM ^[1]
In vitro	ARRY334543 behaves as a reversible ATP-competitive inhibitor with nanomolar potency (Kⁱ=1 nM) both in vitro and in cell-based proliferation assays using A431 and BT-474 cells. ARRY334543 is an AKT pathway inhibitor in cells that contains active ErbB-2 receptors. ARRY334543 suppresses ErbB-2 and ErbB-1 phosphorylation in human cancer cells, such as BT-474 with IC50 of 43 nM) and A431 with IC50 of 36 nM) that overexpress ErbB-2 and ErbB-1, respectively.^[1]
In vivo	When dosed orally, ARRY334543 prevents growth of human tumor xenografts that overexpress ErbB-1 (A431) or ErbB-2 (MDA-MB-453) in a dose-dependent manner. In mouse xenograft models utilizing the EGFR overexpressing tumor line A431, ARRY334543 demonstrates significant dose related tumor growth prevention when administered orally, BID, for 21 days. ARRY334543 has very good in vivo and in vitro PK/ADME properties and has shown excellent activity in numerous mouse tumor xenograft models including epidermoid (A431), breast (BT-474, MDA-MB-453), non-small cell lung (H1650, A549, 292), colorectal (Lovo, HT-29) and gastric (N87) carcinoma models. In the BT-474 model, ARRY334543 demonstrates significant dose-related tumor growth inhibition (69% at 100 mg/kg/d and 98% at 200 mg/kg/d) with significant regressions at both dose levels. Excellent single agent activity for ARRY334543 in the SK-OV-3 ovarian carcinoma xenograft model as well as additive acitivity to trastuzumab in SK-OV-3, BT-474 and NCI-N87 models has been demonstrated. In the BT-474 model, ARRY334543 displays excellent additive activity and tolerability with docetaxel. ^[2]
Features

Protocol(Only for Reference)

Animal Study: ^[2]

Animal Models	Athymic Ncr:Nu/Nu
Dosages	200 mg/kg/d
Administration	Administered via p.o.

References

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

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT00637702	Completed	Advanced Cancer	Array BioPharma	2008-02	Phase 1
NCT00710736	Completed	Advanced Cancer	Array BioPharma	2008-06	Phase 1
NCT00833326	Completed	Advanced Cancer	Array BioPharma	2009-01	Phase 1
NCT00862524	Completed	Advanced Cancer\|Pancreatic Cancer	Array BioPharma	2009-03	Phase 1\|Phase 2
NCT01614522	Recruiting	Stomach Neoplasms\|Cancer of Stomach\|Cancer of the Stomach\|Gastric Cancer\|Gastric Neoplasms	Aslan Pharmaceuticals	2012-03	Phase 2

Chemical Information

Download Varlitinib SDF

Molecular Weight (MW)	466.94
Formula	C₂₂H₁₉ClN₆O₂S
CAS No.	845272-21-1

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

Solubility (25°C) *	In vitro	DMSO	6 mg/mL (12 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.