TAS6417
TAS6417 Basic information
- Product Name:
- TAS6417
- Synonyms:
-
- TAS6417
- TAS-6417;TAS 6417;TAS6417
- (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]-
- CLN-081
- TAS6417 TAS-6417
- Propenamide, N-[(8S)-4-amino-8,9-dihydro-6-methyl-5-(3-quinolinyl)pyrimido[5,4-b]indolizin-8-yl]- (ACI)
- Zipalertinib (TAS-6417)
- CAS:
- 1661854-97-2
- MF:
- C23H20N6O
- MW:
- 396.44
- Product Categories:
-
- API
- APIs
- Mol File:
- 1661854-97-2.mol
TAS6417 Chemical Properties
- Boiling point:
- 756.6±60.0 °C(Predicted)
- Density
- 1.40±0.1 g/cm3(Predicted)
- storage temp.
- 4°C, protect from light, stored under nitrogen
- solubility
- DMSO:20.0(Max Conc. mg/mL);50.44(Max Conc. mM)
- form
- Solid
- pka
- 12.81±0.40(Predicted)
- color
- White to yellow
- InChIKey
- MKCYPWYURWOKST-INIZCTEOSA-N
- SMILES
- C(N[C@H]1C=C(C)C2N(C1)C1=NC=NC(N)=C1C=2C1=CC2C(N=C1)=CC=CC=2)(=O)C=C
TAS6417 Usage And Synthesis
Uses
Zipalertinib (TAS6417; CLN-081) is a highly effective, orally active and pan-mutation-selective EGFR tyrosine kinase inhibitor with a unique scaffold fitting into the ATP-binding site of the EGFR hinge region, with IC50 values ranging from 1.1-8.0 nM[1][2].
in vivo
Zipalertinib (TAS6417) (10-200 mg/kg) causes persistent tumor regression in vivo in EGFR exon 20 insertion-driven tumor models. TAS6417 inhibits mutant EGFR in tumors but not WT EGFR in skin tissues[1].
?
Zipalertinib (TAS6417) had no effect on EGFR-independent proliferation in NCI-H23 or NCI-H460 cells[1].
?
Zipalertinib (TAS6417) administered at 20 mg/kg, which achieves complete suppression of tumor growth, induces a significant decrease in pEGFR, leading to reduction of pAKT and pERK at 1 h. The inhibitory effect is still noted at 6 h, and phosphorylation of EGFR, ATK, and ERK recovered by 24 h[1].
?
Zipalertinib (TAS6417) (100 and 200 mg/kg/day) prolongs survival of animals bearing lung cancer[1].
| Animal Model: | Mice implanted with NCI-H1975 EGFR D770_N771insSVD xenografts[1]. |
| Dosage: | 50 and 100 mg/kg. |
| Administration: | Orally once daily for 14 days. |
| Result: | Showed marked tumor growth inhibition with treatment/control (T/C) ratios of 51% and 19%, respectively. |
IC 50
EGFR: 1.1-8.0 nM (IC50)
References
[1] Hasako S, et al. TAS6417, A Novel EGFR Inhibitor Targeting Exon 20 Insertion Mutations. Mol Cancer Ther. 2018 Aug;17(8):1648-1658. DOI:10.1158/1535-7163.MCT-17-1206
[2] Hibiki Udagawa, et al. TAS6417/CLN-081 Is a Pan-Mutation-Selective EGFR Tyrosine Kinase Inhibitor with a Broad Spectrum of Preclinical Activity against Clinically Relevant EGFR Mutations. Mol Cancer Res. 2019 Nov;17(11):2233-2243. DOI:10.1158/1541-7786.MCR-19-0419
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