1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR

Varlitinib (Synonyms: ARRY-334543)

Cat. No.: HY-10530 Purity: 98.87%
Data Sheet SDS Handling Instructions

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

For research use only. We do not sell to patients.
Varlitinib Chemical Structure

Varlitinib Chemical Structure

CAS No. : 845272-21-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO $132 In-stock
5 mg $120 In-stock
10 mg $190 In-stock
50 mg $540 In-stock
100 mg $740 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

Varlitinib is a selective and potent ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively. IC50 value: 2 nM (ErbB2), 7 nM (ErbB1) Target: ErbB in vitro: Varlitinib is an orally bioavailable inhibitor of the epidermal growth factor receptor family with potential antineoplastic activity. Varlitinib selectively and reversibly binds to both EGFR (ErbB-1) and Her-2/neu (ErbB-2) and prevents their phosphorylation and activation, which may result in inhibition of the associated signal transduction pathways, inhibition of cellular proliferation and cell death. EGFR and Her-2 play important roles in cell proliferation and differentiation and are upregulated in various human tumor cell types. Due to the dual inhibition of both EGFR and Her-2, this agent may be therapeutically more effective than agents that inhibit EGFR or Her-2 alone. 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.

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00637702 Array BioPharma Advanced Cancer February 2008 Phase 1
NCT00278902 Array BioPharma Advanced Cancer January 2006 Phase 1
NCT00710736 Array BioPharma Advanced Cancer June 2008 Phase 1
NCT00862524 Array BioPharma Advanced Cancer|Pancreatic Cancer March 2009 Phase 1|Phase 2
NCT00833326 Array BioPharma Advanced Cancer January 2009 Phase 1
NCT00637702 Array BioPharma Advanced Cancer February 2008 Phase 1
NCT00278902 Array BioPharma Advanced Cancer January 2006 Phase 1
NCT00710736 Array BioPharma Advanced Cancer June 2008 Phase 1
NCT00862524 Array BioPharma Advanced Cancer|Pancreatic Cancer March 2009 Phase 1|Phase 2
NCT00833326 Array BioPharma Advanced Cancer January 2009 Phase 1
NCT03129074 Aslan Pharmaceuticals Advanced or Metastatic Biliary Tract Cancer July 2017 Phase 2
NCT02992340 Aslan Pharmaceuticals Biliary Tract Cancer November 2016 Phase 1|Phase 2
NCT03093870 Aslan Pharmaceuticals Biliary Tract Cancer May 24, 2017 Phase 2|Phase 3
NCT03082053 Aslan Pharmaceuticals Advanced or Metastatic Biliary Tract Cancer|Advanced or Metastatic Solid Tumors January 31, 2017 Phase 1
NCT03130790 Aslan Pharmaceuticals Gastric Cancer September 2017 Phase 2|Phase 3
NCT02609958 Aslan Pharmaceuticals Cholangiocarcinoma October 2015 Phase 2
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Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.1416 mL 10.7080 mL 21.4160 mL
5 mM 0.4283 mL 2.1416 mL 4.2832 mL
10 mM 0.2142 mL 1.0708 mL 2.1416 mL
Molecular Weight

466.94

Formula

C₂₂H₁₉ClN₆O₂S

CAS No.

845272-21-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 16.67 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Varlitinib
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HY-10530
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