| Identification | Back Directory | [Name]
ARRY-334543 | [CAS]
845272-21-1 | [Synonyms]
Varlitinib
ARRY-334543
AR-00334543
Varlitinib Ditosylate
Varlitinib ARRY 334543
ARRY 334543 (Varlitinib)
(R)-N4-(3-Chloro-4-(thiazol-2-ylmethoxy)phenyl)-N6-(4-methyl-4,5-dihydrooxazol-2-yl)quinazolin
(R)-N4-(3-chloro-4-(thiazol-2-ylmethoxy)phenyl)-N6-(4-methyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine
N4-[3-chloro-4-(2-thiazolylmethoxy)phenyl]-N6-[(4R)-4,5-dihydro-4-methyl-2-oxazolyl]-4,6-Quinazoline diamine
(R)-4-[[3-Chloro-4-[(thiazol-2-yl)methoxy]phenyl]amino]-6-[(4-methyl-4,5-dihydrooxazol-2-yl)amino]quinazoline | [Molecular Formula]
C22H19ClN6O2S | [MDL Number]
MFCD20275099 | [MOL File]
845272-21-1.mol | [Molecular Weight]
466.943 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [Uses]
ARRY334543 is a selective and potent ErbB1 and ErbB2 inhibitor with IC50 of 7 nM and 2 nM, respectively. | [Uses]
Varlitinib is a tyrosine kinase inhibitor being developed for the treatment of cancer. Varlitinib acts by disrupting the receptor tyrosine kinases ErbB-2, ErbB-4 and EGFR. | [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) | [storage]
Store at -20°C |
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| Company Name: |
NCE Biomedical Co.,Ltd.
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| Tel: |
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15748/0_EN.htm |
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