1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. Varlitinib

Varlitinib (Synonyms: ASLAN001; ARRY-334543)

Cat. No.: HY-10530 Purity: >98.0%
Handling Instructions

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

For research use only. We do not sell to patients.

Varlitinib Chemical Structure

Varlitinib Chemical Structure

CAS No. : 845272-21-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 123 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 190 In-stock
Estimated Time of Arrival: December 31
50 mg USD 470 In-stock
Estimated Time of Arrival: December 31
100 mg USD 780 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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Description

Varlitinib (ASLAN001) is a potent, reversible, small molecule pan-EGFR inhibitor with IC50s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively[1].

IC50 & Target[1]

HER1

7 nM (IC50)

HER2

2 nM (IC50)

HER4

4 nM (IC50)

In Vitro

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[2].

In Vivo

Varlitinib treatment potently inhibits tumor growth with complete tumor regression observed at dosing of 100 mg/kg twice a day. After five days of Varlitinib treatment, phosphorylation of HER1-3, RAS/RAF/MEK/MAPK, p70S6K, S6 ribosomal, 4EBP1, Cdk-2, Cdc-2 and retinoblastoma are strongly inhibited. Varlitinib treatment results in a significant reduction in survivin and a concomittant increase in Caspase 3 cleavage products[1]. In murine xenograft models, Varlitinib (ARRY-334543) demonstrates significant dose-related (25, 50, 100 mg/kg) tumor growth inhibition in A431-derived tumors when administered orally, twice a day, for 21 days[2].

Clinical Trial
Molecular Weight

466.94

Formula

C₂₂H₁₉ClN₆O₂S

CAS No.

845272-21-1

SMILES

C[[email protected]]1N=C(NC2=CC3=C(NC4=CC=C(OCC5=NC=CS5)C(Cl)=C4)N=CN=C3C=C2)OC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (107.08 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1416 mL 10.7080 mL 21.4160 mL
5 mM 0.4283 mL 2.1416 mL 4.2832 mL
10 mM 0.2142 mL 1.0708 mL 2.1416 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.35 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.35 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Mice: 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

VarlitinibASLAN001ARRY-334543ASLAN 001ASLAN-001ARRY334543ARRY 334543EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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Varlitinib
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