- Varlitinib
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- $0.00 / 1KG
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2025-04-04
- CAS:845272-21-1
- Min. Order: 1KG
- Purity: 98%
- Supply Ability: 1Ton
- Varlitinib
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- $30.00 / 1mg
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2024-11-19
- CAS:845272-21-1
- Min. Order:
- Purity: 99.7%
- Supply Ability: 10g
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| | 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);N4-[3-chloro-4-(2-thiazolylmethoxy)phenyl]-N6-[(4R)-4,5-dihydro-4-methyl-2-oxazolyl]-4,6-Quinazoline diamine | | CAS: | 845272-21-1 | | MF: | C22H19ClN6O2S | | MW: | 466.94 | | EINECS: | | | 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) |
| | ARRY-334543 Preparation Products And Raw materials |
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