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Varlitinib

Catalog No. T6719 CAS 845272-21-1

Synonyms: ASLAN001, ARRY-334543

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

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Varlitinib, CAS 845272-21-1

Pack Size	Availability	Price/USD
2 mg	In stock	$ 67.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 172.00
25 mg	In stock	$ 288.00
1 mL * 10 mM (in DMSO)	In stock	$ 111.00

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Purity: 99.7%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Varlitinib (ASLAN001) is a potent, reversible, small molecule pan-EGFR inhibitor with IC50s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively.
Targets&IC50	ERB1:7 nM, ErbB2:2 nM
In vitro	In cell-based assays involving tumor cells with over-expression of EGFR (A431) or ErbB-2 (BT474), Varlitinib (ARRY-334543) effectively inhibits substrate phosphorylation and demonstrates high selectivity for EGFR/ErbB-2 without significant activity against a panel of 104 other kinases[2].
In vivo	Varlitinib treatment effectively suppresses tumor growth, achieving complete tumor regression at a dosage of 100 mg/kg administered twice daily. Within five days of treatment, Varlitinib significantly inhibits the phosphorylation of key signaling molecules including HER1-3, RAS/RAF/MEK/MAPK, p70S6K, S6 ribosomal protein, 4EBP1, Cdk-2, Cdc-2, and retinoblastoma. This inhibition is accompanied by a marked decrease in survivin levels and an increase in Caspase 3 cleavage products, indicating enhanced apoptosis. Additionally, in murine xenograft models, Varlitinib (ARRY-334543) shows substantial, dose-dependent tumor growth inhibition in A431-derived tumors when given orally at doses of 25, 50, and 100 mg/kg, twice a day for 21 days.

Synonyms	ASLAN001, ARRY-334543
Molecular Weight	466.94
Formula	C22H19ClN6O2S
CAS No.	845272-21-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 31.5 mg/mL (67.5 mM), Sonication and heating to 60℃ are recommended.

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

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

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Clinical Compound Library Bioactive Compound Library Anti-Pancreatic Cancer Compound Library Anti-Breast Cancer Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Varlitinib 845272-21-1 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors HER ARRY 334543 ASLAN001 ARRY-334543 ARRY334543 ASLAN-001 ASLAN 001 inhibitor inhibit

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