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Datasheet of Varlitinib

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

Chemical Information
Catalog

DC8486

Purity of current batch:

>98%

Molecular Weight (MW)

466.94326

Molecular Formula

C22H19ClN6O2S

CAS No.

845272-21-1

Solubility (25C)

DMSO

Storage

Store at -20C (desiccating conditions).

Handling:
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in
advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable
for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room
temperature for at least 1 hour.