country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-10530A

Copy Link Print Information

Varlitinib tosylate

(Synonyms: ASLAN001 tosylate; ARRY-334543 tosylate)

2 Cited Publications

Customer Review

Based on 2 publication(s) in Google Scholar

Varlitinib (ASLAN001) tosylate is a potent, reversible, small molecule pan-EGFR inhibitor with IC₅₀s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively.

For research use only. We do not sell to patients.

CAS No.: 1146629-86-8
Formula: C₃₆H₃₅ClN₆O₈S₃
Molecular Weight:811.35

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (277 KB)

Varlitinib tosylate Chemical Structure

CAS No.: 1146629-86-8

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (2)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Varlitinib (ASLAN001) tosylate is a potent, reversible, small molecule pan-EGFR inhibitor with IC₅₀s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively^[1].

IC₅₀ & Target

IC50: 7 nM (HER1), 2 nM (HER2), 4 nM (HER4)^[1]

All EGFR Isoforms :

In Vitro

In cell-based assays using tumor cells that over-express EGFR (A431) or ErbB-2 (BT474), Varlitinib tosylate (ARRY-334543) potently inhibits substrate phosphorylation. Varlitinib tosylate is shown to be highly selective for EGFR/ErbB-2, and does not show any significant activity when screened against a panel of 104 kinases^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Varlitinib tosylate treatment potently inhibits tumor growth with complete tumor regression observed at dosing of 100 mg/kg twice a day. After five days of Varlitinib tosylate treatment, phosphorylation of HER1-3, RAS/RAF/MEK/MAPK, p70S6K, S6 ribosomal, 4EBP1, Cdk-2, Cdc-2 and retinoblastoma are strongly inhibited. Varlitinib tosylate treatment results in a significant reduction in survivin and a concomittant increase in Caspase 3 cleavage products^[1]. In murine xenograft models, Varlitinib tosylate (ARRY-334543) demonstrates significant dose-related (25, 50, 100 mg/kg) tumor growth inhibition in A431-derived tumors when administered orally, twice a day, for 21 days^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1146629-86-8
Molecular Weight 811.35
Formula C₃₆H₃₅ClN₆O₈S₃
SMILES

C[C@H]1N=C(NC2=CC3=C(NC4=CC=C(OCC5=NC=CS5)C(Cl)=C4)N=CN=C3C=C2)OC1.O=S(C6=CC=C(C=C6)C)(O)=O.O=S(C7=CC=C(C=C7)C)(O)=O
Synonyms

ASLAN001 tosylate; ARRY-334543 tosylate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (2)

All

Sort by:

Journal Impact Factor

Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Adv Sci (Weinh)

Amphiregulin and Epiregulin Confer Radioresistance in Esophageal Squamous Cell Carcinoma Through Oxidative Phosphorylation. [Abstract]

2025 Nov 9:e07524. PMID: 41208199

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Hsieh C, et al. Varlitinib to demonstrate anti-tumour efficacy in patient-derived hepatocellular carcinoma xenograft models. Journal of Clinical Oncology 34, no. 15_suppl

[2]. Miknis G, et al. ARRY-334543, A potent, orally active small molecule inhibitor of EGFR and ErbB-2.Proc Amer Assoc Cancer Res, Volume 46, 2005

Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

Varlitinib tosylate

2 Cited Publications

100 mg Get Quote

Subscribe to the

MedChemExpress

Newsletter

MOQ

Minimum order quantity

100 mg

Get Quote In-stock

Other size

Get Quote

Amount: USD 0.00

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (2)
Purity & Documentation
References

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

Varlitinib tosylate

Publications Citing Use of MedChemExpress (MCE) Varlitinib tosylate

All EGFR Isoforms

Biological Activity

Chemical Information

Publications (2)

Purity & Documentation

References

Calculators

Help & FAQs

Varlitinib tosylate Related Classifications

HY-10530A Related Classifications