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

Varlitinib (Synonyms: ARRY-334543)

Cat. No.: HY-10530 Purity: 98.87%
Data Sheet SDS 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 $132 In-stock
5 mg $120 In-stock
10 mg $190 In-stock
50 mg $540 In-stock
100 mg $740 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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.

IC50 & Target

IC50: 7 nM (HER1), 2 nM (HER2), 4 nM (HER4)[1]

In Vitro

In cell-based assays using tumor cells that over-express EGFR (A431) or ErbB-2 (BT474), Varlitinib 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 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
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References
Preparing Stock Solutions
Concentration Volume 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.
Animal Administration
[1]

Mouse: 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
Molecular Weight

466.94

Formula

C₂₂H₁₉ClN₆O₂S

CAS No.

845272-21-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 16.67 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Varlitinib
Cat. No.:
HY-10530
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