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| | ARRY-543 Basic information |
| Product Name: | ARRY-543 | | Synonyms: | N4-[3-Chloro-4-(2-thiazolylmethoxy)phenyl]-N6-[(4R)-4,5-dihydro-4-methyl-2-oxazolyl]-4,6-quinazolinediamine 4-methylbenzenesulfonate;Varlitinib tosylate;ARRY-543 TOSYLATE;N4-[3-chloro-4-(2-thiazolylmethoxy)phenyl]-N6-[(4R)-4,5-dihydro-4-methyl-2-oxazolyl]-4,6-Quinazolinediaminebis(4-methylbenzenesulfonate);Arry-543 tosylate (1:2);ARRY-334543 Tosylate;Varlitinib tosylate (ASLAN001 tosylate, ARRY-334543 tosylate) | | CAS: | 1146629-86-8 | | MF: | C29H27ClN6O5S2 | | MW: | 639.14488 | | EINECS: | | | Product Categories: | | | Mol File: | 1146629-86-8.mol |  |
| | ARRY-543 Chemical Properties |
| | ARRY-543 Usage And Synthesis |
| Uses | ARRY334543 is a selective and potent ErbB1 and ErbB2 inhibitor with IC50 of 7 nM and 2 nM, respectively. | | in vivo | Varlitinib tosylate treatment potently inhibits tumor growth with complete tumor regression observed at dosing of 100 mg/kg twice a day. After five days of Varlitinib tosylate treatment, phosphorylation of HER1-3, RAS/RAF/MEK/MAPK, p70S6K, S6 ribosomal, 4EBP1, Cdk-2, Cdc-2 and retinoblastoma are strongly inhibited. Varlitinib tosylate treatment results in a significant reduction in survivin and a concomittant increase in Caspase 3 cleavage products[1]. In murine xenograft models, Varlitinib tosylate (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]. |
| | ARRY-543 Preparation Products And Raw materials |
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