For research use only.
Catalog No.S2755 Synonyms: ARRY334543
CAS No. 845272-21-1
Varlitinib (ARRY334543) is a selective and potent ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively. Phase 2.
Selleck's Varlitinib has been cited by 6 publications
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Reversal effect of ARRY-334543 on the sensitivity of HEK/MRP7 cells to vincristine. The figure showes the survival curves of cells at different concentrations of vincristine with or without ARRY-334543. Cell viability was determined by MTT Assay. HEK293 is human embryonic kidney cell line while HEK/MRP7 is MRP7-transfected cell line. Cepharanthine was used as a positive control of MRP7 inhibitor.
Varlitinib purchased from Selleck.
Reversal effect of ARRY-334543 on the sensitivity of HEK293-ABCG2-R2 cells to mitoxantrone. The figure showes the survival curves of cells at different concentrations of mitoxantrone with or without ARRY-334543. Cell viability was determined by MTT Assay. HEK293 is human embryonic kidney cell line while HEK293-ABCG2-R2 is ABCG2-transfected cell line. Nilotinib was used as a positive control of ABCG2 inhibitor.
Varlitinib purchased from Selleck.
A431 80% confluent 10cm plates, 24hour FBS starvation, then treatment with compounds at 10nM for 30mins, followed by 5 minutes of 0.05ug/ml of EGF. Pellet was sonicated (setting 5, 5 seconds, twice), then quenched with 2XGSB. Loaded 10ul on AnyKD BioRad gel (20mins at 250V), transfered with BioRad Turbo system for 15 minutes (1.5A, 25V). Blocked with 5% milk for 1 hour at RT. Rocked overnight at 1:1000 in 5% BSA with primary Abs; Anti-rabbit secondary Ab at 1:2000 in 5% milk for 1 hour, developed with Thermo Femto Kit.
Varlitinib purchased from Selleck.
Purity & Quality Control
Choose Selective EGFR Inhibitors
|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.|
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.
|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. |
|In vitro||DMSO||6 mg/mL (12.84 mM)|
* 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03231176||Completed||Drug: Varlitinib|Drug: Capecitabine||Biliary Tract Cancer||Aslan Pharmaceuticals||December 19 2017||Phase 2|
|NCT03368846||Completed||Drug: Varlitinib||Healthy Volunteers||Aslan Pharmaceuticals||November 23 2017||Phase 1|
|NCT02992340||Terminated||Drug: Varlitinib|Drug: Cisplatin|Drug: Gemcitabine||Biliary Tract Cancer||Aslan Pharmaceuticals||December 13 2016||Phase 1|Phase 2|
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.
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