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Varlitinib

Cat. No. M3199

Varlitinib Structure
Size Price Availability Quantity
5mg USD 220 In stock
10mg USD 300 In stock
50mg USD 860 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

ARRY334543 is a selective and potent kinase ErbB-1 and ErbB-2 inhibitor with IC50 of 7 and 2 nM, respectively. The Ki of ARRY334543 is 1 nM. ARRY334543 behaves as a reversible ATP-competitive inhibitor with nanomolar potency 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 an IC50 of 43 nM and A431 with an IC50 of 36 nM that overexpress ErbB-2 and ErbB-1, respectively. When dosed orally, ARRY334543 dose-dpendently inhibits growth of human tumor xenografts that overexpress ErbB-1 (A431) or ErbB-2 (MDA-MB-453). ARRY334543 demonstrates significant dose related tumor growth prevention when administered orally, BID, for 21 days. ARRY334543 has very good PK/ADME properties and has revealed 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 by 69% at 100 mg/kg/d and by 98% at 200 mg/kg/d. Excellent single agent activity for ARRY334543 in the SK-OV-3 ovarian carcinoma xenograft model as well as additive activity to trastuzumab in SK-OV-3, BT-474 and NCI-N87 models has been demonstrated. ARRY334543 exhibits excellent additive activity and tolerability with docetaxel. ARRY334543 is carried out in a phase II clinical trial in the treatment of advanced cancer and pancreatic cancer.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Athymic Ncr:Nu/Nu
Formulation
Dosages 200 mg/kg/d
Administration Administered via p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 466.94
Formula C22H19ClN6O2S
CAS Number 845272-21-1
Purity >99%
Solubility DMSO
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Varlitinib supplier, EGFR/HER2, inhibitors

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