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Varlitinib (ARRY334543)

ErbB inhibitor CAS# 845272-21-1

Varlitinib (ARRY334543)

Catalog No. BCC3725----Order now to get a substantial discount!

Product Name & Size Price Stock
Varlitinib (ARRY334543): 5mg $127 In Stock
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Chemical structure

Varlitinib (ARRY334543)

3D structure

Chemical Properties of Varlitinib (ARRY334543)

Cas No. 845272-21-1 SDF Download SDF
PubChem ID 42642648 Appearance Powder
Formula C22H19ClN6O2S M.Wt 466.94
Type of Compound N/A Storage Desiccate at -20°C
Synonyms ARRY-334543
Solubility DMSO : 50 mg/mL (107.08 mM; Need ultrasonic)
Chemical Name 4-N-[3-chloro-4-(1,3-thiazol-2-ylmethoxy)phenyl]-6-N-[(4R)-4-methyl-4,5-dihydro-1,3-oxazol-2-yl]quinazoline-4,6-diamine
SMILES CC1COC(=N1)NC2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=NC=CS5)Cl
Standard InChIKey UWXSAYUXVSFDBQ-CYBMUJFWSA-N
Standard InChI 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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Varlitinib (ARRY334543)

DescriptionVarlitinib is a selective and potent inhibitor of ErbB1(EGFR) and ErbB2(HER2) with IC50 values of 7 nM and 2 nM, respectively.
TargetsErbB2ErbB1    
IC502 nM7 nM    

Varlitinib (ARRY334543) Dilution Calculator

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Varlitinib (ARRY334543) Molarity Calculator

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Preparing Stock Solutions of Varlitinib (ARRY334543)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.1416 mL 10.708 mL 21.416 mL 42.8321 mL 53.5401 mL
5 mM 0.4283 mL 2.1416 mL 4.2832 mL 8.5664 mL 10.708 mL
10 mM 0.2142 mL 1.0708 mL 2.1416 mL 4.2832 mL 5.354 mL
50 mM 0.0428 mL 0.2142 mL 0.4283 mL 0.8566 mL 1.0708 mL
100 mM 0.0214 mL 0.1071 mL 0.2142 mL 0.4283 mL 0.5354 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Varlitinib (ARRY334543)

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.

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Description

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

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