TAS6417

Name	TAS6417
Synonyms	CLN-081 TAS6417 TAS 6417 TAS-6417 1661854-97-2 TAS6417(CLN-081) TAS6417 TAS-6417 Zipalertinib (TAS-6417) (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]- Propenamide, N-[(8S)-4-amino-8,9-dihydro-6-methyl-5-(3-quinolinyl)pyrimido[5,4-b]indolizin-8-yl]- (ACI)
CAS	1661854-97-2

Molecular Formula	C23H20N6O
Molar Mass	396.44
Density	1.40±0.1 g/cm3(Predicted)
Boling Point	756.6±60.0 °C(Predicted)
pKa	12.81±0.40(Predicted)
Storage Condition	-20℃
In vitro study	In addition to EGFR, TAS6417 also inhibited the other 25 kinases at concentrations below 255 nM, and the IC50 value was more than 1000 times that of WT EGFR. TAS6417 inhibits TXK, BMX, HER4, TEC, BTK and JAK3, with IC50 values less than 10-fold that of WT EGFR. TAS6417 can inhibit the proliferation of Ba/F3 cells driven by a variety of EGFR exon 20 mutations, with IC50 between 5.05±1.33 nmol/L and 150±53 nmol/L. TAS6417 had no effect on EGFR-independent cells, such as NCI-H23 and NCI-H460 cells.
In vivo study	TAS6417 can cause sustained tumor regression in a tumor model driven by EGFR exon 20 insertion mutations. After TAS6417 administration, the tumor regression effect was rapidly generated and effective throughout the treatment. Pharmacokinetic Study analysis showed that after oral administration of 50 mg/kg and 100 mg/kg TAS6417 in mice, the plasma concentration of the drug will decrease rapidly within 4 hours. The effective dose of TAS6417 in rats can achieve the peak blood concentration is lower than in mice, but in the rat model, the blood concentration is more durable and stable, sustainable for up to 8 hours. In skin tissue, TAS6417 can inhibit mutant EGFR rather than wild-type EGFR in tumor tissue. TAS6417 can prolong the survival time of animals with lung cancer.

Last Update：2024-01-02 23:10:35

Last Update：2024-04-09 01:59:50

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Product Name: Zipalertinib Request for quotation
CAS: 1661854-97-2
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052

Wechat: 15671228036

Spot supply

Product Name: TAS6417 Visit Supplier Webpage Request for quotation
CAS: 1661854-97-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

Wechat: 18301782025

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TAS6417

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