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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $89 | In Stock | |
2 mg | $126 | In Stock | |
5 mg | $198 | In Stock | |
10 mg | $328 | In Stock | |
25 mg | $663 | In Stock | |
50 mg | $1,060 | In Stock | |
100 mg | $1,630 | In Stock | |
500 mg | $3,280 | In Stock | |
1 mL x 10 mM (in DMSO) | $226 | In Stock |
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] |
Molecular Weight | 396.44 |
Formula | C23H20N6O |
Cas No. | 1661854-97-2 |
Storage | keep 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
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