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TAS6417

Catalog No. T16996Cas No. 1661854-97-2

Zipalertinib (TAS6417, CLN-081) is a novel, highly potent, orally active covalent EGFR tyrosine kinase inhibitor that uniquely binds to the ATP binding site of the EGFR hinge region with an IC50 value of 1.1-8.0 nM.

TAS6417

TAS6417

Purity: 99.19%
Catalog No. T16996Cas No. 1661854-97-2
Zipalertinib (TAS6417, CLN-081) is a novel, highly potent, orally active covalent EGFR tyrosine kinase inhibitor that uniquely binds to the ATP binding site of the EGFR hinge region with an IC50 value of 1.1-8.0 nM.
Pack SizePriceAvailabilityQuantity
1 mg$89In Stock
2 mg$126In Stock
5 mg$198In Stock
10 mg$328In Stock
25 mg$663In Stock
50 mg$1,060In Stock
100 mg$1,630In Stock
500 mg$3,280In Stock
1 mL x 10 mM (in DMSO)$226In Stock
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Purity:99.19%
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Product Introduction

Bioactivity
Description
Zipalertinib (TAS6417, CLN-081) is a novel, highly potent, orally active covalent EGFR tyrosine kinase inhibitor that uniquely binds to the ATP binding site of the EGFR hinge region with an IC50 value of 1.1-8.0 nM.
Targets&IC50
EGFR:1.1-8.0 nM
In vitro
METHODS: Two cell lines with EGFR exon 20 insertion isolated and established from lung cancer patients, BID007 and BID019, were treated with Zipalertinib (TAS6417, CLN-081) (0.001, 0.01, 0.1, 1, 10 μM).
RESULTS Zipalertinib (TAS6417, CLN-081) inhibited EGFR phosphorylation in both cell lines at 10 nM and 100 nM. [1]
In vivo
METHODS: Nude mice bearing NIH/3T3 EGFR G719A allografts, nude mice bearing BID007, and nude mice bearing H1975 cells were treated with TAS6417 (50, 100, 200 mg/kg, oral, 15 days) to study the in vivo efficacy of Zipalertinib (TAS6417, CLN-081) against EGFR mutations.
RESULTS Zipalertinib (TAS6417, CLN-081) inhibited tumor formation in nude mice bearing H1975, NIH/3T3 expressing G719A, NIH/3T3 expressing G719A+T790M, BID007, and H1975-insSVD. [1]
Chemical Properties
Molecular Weight396.44
FormulaC23H20N6O
Cas No.1661854-97-2
Storage & Solubility Information
Storagekeep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 55 mg/mL (138.73 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.5224 mL12.6122 mL25.2245 mL126.1225 mL
5 mM0.5045 mL2.5224 mL5.0449 mL25.2245 mL
10 mM0.2522 mL1.2612 mL2.5224 mL12.6122 mL
20 mM0.1261 mL0.6306 mL1.2612 mL6.3061 mL
50 mM0.0504 mL0.2522 mL0.5045 mL2.5224 mL
100 mM0.0252 mL0.1261 mL0.2522 mL1.2612 mL

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