ARRY-334543
ARRY-334543 Basic information
- Product Name:
- ARRY-334543
- Synonyms:
-
- ARRY-334543
- AR-00334543
- Varlitinib
- (R)-4-[[3-Chloro-4-[(thiazol-2-yl)methoxy]phenyl]amino]-6-[(4-methyl-4,5-dihydrooxazol-2-yl)amino]quinazoline
- (R)-N4-(3-chloro-4-(thiazol-2-ylmethoxy)phenyl)-N6-(4-methyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine
- Varlitinib ARRY 334543
- ARRY 334543 (Varlitinib)
- ASLAN001)
- CAS:
- 845272-21-1
- MF:
- C22H19ClN6O2S
- MW:
- 466.94
- Product Categories:
-
- Inhibitors
- Mol File:
- 845272-21-1.mol
ARRY-334543 Chemical Properties
- Boiling point:
- 637.1±65.0 °C(Predicted)
- Density
- 1.51±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 50 mg/mL (107.08 mM; Need ultrasonic)
- form
- Powder
- pka
- 6.54±0.70(Predicted)
- color
- Off-white to yellow
- CAS DataBase Reference
- 845272-21-1
ARRY-334543 Usage And Synthesis
Uses
ARRY334543 is a selective and potent ErbB1 and ErbB2 inhibitor with IC50 of 7 nM and 2 nM, respectively.
Enzyme inhibitor
This ErbB1/2 inhibitor (FW = 466.94 g/mol; CAS 845272-21-1), also named (R)-N4 -(3-chloro-4-(thiazol-2-ylmethoxy)phenyl)-N6 -(4-methyl-4,5- dihydrooxazol-2-yl)quinazoline-4,6-diamine, selectively targets the intrinsic protein kinase activities of ErbB1, or Epidermal Growth Factor Receptor (EGFR), IC50 = 7 nM and ErbB2, or Human Epidermal growth factor Receptor (HER2), IC50 = 2 nM. ARRY-334543 also reverses multidrug resistance by antagonizing the activity of ATP-binding cassette subfamily G member 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].
target
ErbB2
IC 50
HER1: 7 nM (IC50); HER2: 2 nM (IC50); HER4: 4 nM (IC50)
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