Home Protein Tyrosine Kinase EGFR inhibitor Varlitinib For research use only.

Varlitinib

Synonyms: ARRY334543

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

Varlitinib Chemical Structure

Varlitinib Chemical Structure

CAS No. 845272-21-1

Purity & Quality Control

Varlitinib Related Products

Signaling Pathway

EGFR Signaling Pathways

EGFR Signaling Pathway

Biological Activity

Description Varlitinib (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 [1]
(Cell-free assay)		 ErbB1 [1]
(Cell-free assay)
2 nM 7 nM
In vitro
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
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]
Animal Research Animal Models Athymic Ncr:Nu/Nu
Dosages 200 mg/kg/d
Administration Administered via p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03231176 Completed
Biliary Tract Cancer
ASLAN Pharmaceuticals
 December 19 2017 Phase 2
NCT03368846 Completed
Healthy Volunteers
ASLAN Pharmaceuticals
 November 23 2017 Phase 1
NCT02992340 Terminated
Biliary Tract Cancer
ASLAN Pharmaceuticals
 December 13 2016 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 466.94 Formula

C22H19ClN6O2S
CAS No. 845272-21-1 SDF Download Varlitinib SDF
Smiles CC1COC(=N1)NC2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=NC=CS5)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 6 mg/mL ( (12.84 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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