845272-21-1
845272-21-1 structure
- Name: Varlitinib
- 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
- CAS Number: 845272-21-1
- Molecular Formula: C22H19ClN6O2S
- Molecular Weight: 466.943
- Catalog: Biochemical Inhibitor Protein tyrosine kinase
- Create Date: 2018-10-18 23:36:14
- Modify Date: 2025-08-25 11:42:44
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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.
| 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 |
|---|---|
| Synonyms |
4,6-Quinazolinediamine, N-[3-chloro-4-(2-thiazolylmethoxy)phenyl]-N-[(4R)-4,5-dihydro-4-methyl-2-oxazolyl]-
ARRY-543 N-[3-Chloro-4-(1,3-thiazol-2-ylmethoxy)phenyl]-N-[(4R)-4-methyl-4,5-dihydro-1,3-oxazol-2-yl]-4,6-quinazolinediamine Varlitinib (USAN/INN) Varlitinib |
| 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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| Related Catalog | |
| Target |
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]. |
| Animal Admin | 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]. |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Boiling Point | 637.1±65.0 °C at 760 mmHg |
| Molecular Formula | C22H19ClN6O2S |
| Molecular Weight | 466.943 |
| Flash Point | 339.1±34.3 °C |
| Exact Mass | 466.097870 |
| PSA | 121.79000 |
| LogP | 3.51 |
| Vapour Pressure | 0.0±1.9 mmHg at 25°C |
| Index of Refraction | 1.742 |
| Storage condition | -20℃ |