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    Varlitinib (ARRY-543; ARRY-334543; ASLAN-001)
    Varlitinib (ARRY-543; ARRY-334543; ASLAN-001)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0570
    CAS #: 845272-21-1Purity ≥98%

    Description: Varlitinib (formerly also known as ARRY543; ARRY-334543; ASLAN001) is a novel, potent, orally bioavailable, selective and reversible ErbB1 (EGFR) and ErbB2 (HER2) inhibitor with potential antitumor activity. It inhibits ErbB1 (EGFR) and ErbB2 (HER2) with IC50 of 7 nM and 2 nM, respectively. 

    References: Abstracts #3399.

    Related CAS: 1146629-86-8 (Varlitinib Tosylate)

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    Molecular Weight (MW)466.94
    FormulaC22H19ClN6O2S
    CAS No.845272-21-1 (free base); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 6 mg/mL (12.8 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other infoChemical Name: (R)-N4-(3-chloro-4-(thiazol-2-ylmethoxy)phenyl)-N6-(4-methyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine.
    InChi Key: UWXSAYUXVSFDBQ-CYBMUJFWSA-N
    InChi Code: InChI=1S/C22H19ClN6O2S/c1-13-10-31-22(27-13)29-14-2-4-18-16(8-14)21(26-12-25-18)28-15-3-5-19(17(23)9-15)30-11-20-24-6-7-32-20/h2-9,12-13H,10-11H2,1H3,(H,27,29)(H,25,26,28)/t13-/m1/s1
    SMILES Code: C[[email protected]]1N=C(NC2=CC3=C(NC4=CC=C(OCC5=NC=CS5)C(Cl)=C4)N=CN=C3C=C2)OC1
    SynonymsARRY334543, ASLAN001; ASLAN-001; ASLAN 001; AR 00334543; ARRY-334543; ARRY543; ARRY-543; ARRY 543 


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    In Vitro

    In vitro activity: 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


    Kinase Assay: Varlitinib (ARRY-334543; ASLAN001) is a novel, potent, reversible, small molecule pan-EGFR inhibitor with IC50s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively.


    Cell Assay: In cell-based assays using tumor cells that over-express EGFR (A431) or ErbB-2 (BT474), Varlitinib (ARRY-334543) potently inhibits substrate phosphorylation. Varlitinib 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

    In VivoWhen 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.
    Animal modelMice: The effects of Varlitinib is tested in patient-derived HCC xenograft in SCID mice (HCC29-0909A) with co-expression of HER1, HER2 and HER3 recepors. Mice are treated with Varlitinib when the tumors reach the size of approximately 100-150 mm3. Tumor size measurements are performed twice a week and tumor volumes are calculated
    Formulation & Dosage100, 200 mg/kg
    ReferencesAbstracts #3399.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Abstracts #3399.

    Varlitinib

    Varlitinib exerts anti-proliferation ability and induces apoptosis in MDA-MB-453 and MDA-MB-468 cells but not MDA-MB-231 cells. Cancers (Basel). 2019 Jan; 11(1): 105.

    Varlitinib

    Varlitinib inhibits MEK/ERK and Akt pathway in TNBC cells. Cancers (Basel). 2019 Jan; 11(1): 105.

    Varlitinib

    ERK signaling mediates varlitinib-induced apoptosis in TNBC cells. Cancers (Basel). 2019 Jan; 11(1): 105.

    Varlitinib

    Varlitinib inhibits tumor growth of TNBC. Cancers (Basel). 2019 Jan; 11(1): 105.

    Varlitinib

    Varlitinib reduces the abilities of migration, invasion and mammosphere formation of TNBC cells. (A–C) MDA-MB-231 and MDA-MB-468 cells were treated with varlitinib or DMSO for subsequent migration (A), invasion (B) and mammosphere assays (C).  Cancers (Basel). 2019 Jan; 11(1): 105.


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