An inhibitor of EGFR and HER2
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Varlitinib

Item No. 27651

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N4-[3-chloro-4-(2-thiazolylmethoxy)phenyl]-N6-[(4R)-4,5-dihydro-4-methyl-2-oxazolyl]-4,6-quinazolinediamine
CAS Number
845272-21-1
Synonyms
  • ARRY-334543
Molecular Formula
C22H19ClN6O2S
Formula Weight
466.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 5 mg/mlEthanol: 0.5 mg/mlPBS (pH 7.2): partially soluble
λmax
244, 303, 356 nm
SMILES
ClC1=C(OCC2=NC=CS2)C=CC(NC3=NC=NC4=C3C=C(NC5=N[C@H](C)CO5)C=C4)=C1
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
InChi Key
UWXSAYUXVSFDBQ-CYBMUJFWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    Product Description

    Varlitinib is an inhibitor of EGFR and HER2 (IC50s = 7 and 2 nM, respectively).1,2 It inhibits cell proliferation (IC50s = <20 μM) and induces apoptosis in MDA-MB-453 and MDA-MB-468 triple-negative breast cancer (TNBC) cells.2 Varlitinib inhibits migration, invasion, and mammosphere formation of MDA-MB-231 and MDA-MB-468 cells. In vivo, varlitinib (100 mg/kg) inhibits phosphorylation of EGFR and ERK and reduces tumor weight in an MDA-MB-468 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Miknis, G., Wallace, E., Lyssikatos, J., et al. ARRY-334543, a potent, orally active, small molecule inhibitor of EGFR and ErbB-2. Cancer Res. 65(9 Suppl.), 801 (2005).

    2. Liu, C.-Y., Chu, P.-Y., Huang, C.-T., et al. Varlitinib downregulates HER/ERK signaling and induces apoptosis in triple negative breast cancer cells. Cancer (Basel) 11(1), E105 (2019).