TAS6417，CAS 1661854-97-2

Product Description:

Product Name: TAS6417,CAS 1661854-97-2

Synonyms:

(S)-N-(4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dihydropyrimido[5,4-b]indolizin-8-yl)acrylamide;

2-Propenamide,N-[(8S)-4-amino-8,9-dihydro-6-methyl-5-(3-quinolinyl)pyrimido[5,4-b]indolizin-8-yl]-;

Chemical & Physical Properties

Assay: NLT99%

Density:1.40±0.1 g/cm³

Molecular Formula:C23H20N6O

Molecular Weight:396.44

Boling Point:756.6±60.0℃

pKa:12.81±0.40

Storage Condition:-20℃

Uses :

Among the 255 detected kinases, in addition to EGFR, TAS6417 also inhibited 25 other kinases at concentrations below 1000nM, with an IC50 value more than 100 times that of WTEGFR. TAS6417 inhibits TXK, BMX, HER4, TEC, BTK, and JAK3, with an IC50 value less than 10 times its IC5Chemicalbook0 value for WTEGFR. TAS6417 can inhibit the proliferation of Ba/F3 cells driven by multiple EGFR Exon 20 mutations, with IC50 ranging from 5.05 ± 1.33 nmol/L to 150 ± 53 nmol/L. TAS6417 has no effect on EGFR independent cells, such as NCI-H23 and NCI-H460 cells.

In the tumor model driven by the insertion mutation of EGFR Exon 20, TAS6417 can cause sustained tumor regression. After the administration of TAS6417, the tumor regression effect rapidly occurs and is effective throughout the entire treatment process. Pharmacokinetic analysis shows that after oral administration of 50mg/kg and 100mg/kg of TAS6417 in mice, the plasma concentration of the drug will rapidly decrease within 4 hours of Chemicalbook. The effective dose of TAS6417 in rats can reach a lower peak blood concentration than that in mice, but the blood concentration in rat models is more persistent and stable, lasting up to 8 hours. In skin tissue, TAS6417 can inhibit Mutant EGFR rather than wild EGFR in tumor tissue. TAS6417 can prolong the survival time of animals with lung cancer.

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