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TAS6417

TAS6417 Structure
TAS6417
TAS6417 Property
  • 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
  • FDA UNII T4YMU8TW9H
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal word
  • Hazard statements
  • Precautionary statements

TAS6417 Chemical Properties,Usage,Production

  • 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
TAS6417 Preparation Products And Raw materials
Raw materials
Preparation Products
TAS6417 Suppliers
Global(103)Suppliers
  • Supplier：
    TargetMol Chemicals Inc.
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    Shanghai UCHEM Inc.
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    LEAPCHEM CO., LTD.
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  • Supplier：
    Aladdin Scientific
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  • Email：tp@aladdinsci.com
  • Country：United States
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TAS6417 Spectrum
1661854-97-2, TAS6417Related Search:
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  • 合成有机化合物配体
  • 实验室
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  • 黄金产品
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  • 新产品
  • 化合物TAS6417,10 MM DMSO 溶液
  • (S)-N-(4-氨基-6-甲基-5-(喹啉-3-基)-8,9-二氢嘧啶并[5,4-B]吲嗪-8-基)丙烯酰胺
  • (S)-N-(4-氨基-6-甲基-5-(喹啉-3-基)-8,9-二氢嘧啶并[5,4-B]中氮茚-8-基)丙烯酰胺
  • 齐帕勒替尼(TAS6417)
  • 齐帕勒替尼
  • (S)-N-[4-氨基-6-甲基-5-(3-喹啉基)-8,9-二氢嘧啶并[5,4-B]吲嗪-8-基]丙烯酰胺
  • TAS6417(CLN-081)
  • 化合物TAS6417
  • 2-丙酰胺,N-[(8S)-4-氨基-8,9-二氢-6-甲基-5-(3-喹啉基)嘧啶[5,4-b]吲哚嗪-8-基]-
  • 1661854-97-2
  • TAS6417/Zipalertinib
  • TAS6417, 10 mM in DMSO
  • N-[(8S)-4-amino-8,9-dihydro-6-methyl-5-(3-quinolinyl)pyrimido[5,4-b]indolizin-8-yl]-2-propenamide
  • (S)-N-[4-Amino-6-methyl-5-(3-quinolyl)-8,9-dihydropyrimido[5,4-b]indolizin-8-yl]acrylamide
  • Zipalertinib
  • TAS-6417,EGFR,ErbB-1,TAS6417,PC-9,lung,Inhibitor,Apoptosis,CLN081,BEAS-2B,CLN 081,cancer,BID007,CLN-081,inhibit,TAS 6417,NSCLC,H1975,Epidermal growth factor receptor,BID019,HER1,Akt
  • 2-Propenamide, N-[(8S)-4-amino-8,9-dihydro-6-methyl-5-(3-quinolinyl)pyrimido[5,4-b]indolizi
  • Zipalertinib (TAS-6417)
  • Propenamide, N-[(8S)-4-amino-8,9-dihydro-6-methyl-5-(3-quinolinyl)pyrimido[5,4-b]indolizin-8-yl]- (ACI)
  • TAS6417 TAS-6417
  • CLN-081
  • 2-Propenamide, N-[(8S)-4-amino-8,9-dihydro-6-methyl-5-(3-quinolinyl)pyrimido[5,4-b]indolizin-8-yl]-
  • (S)-N-(4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dihydropyrimido[5,4-b]indolizin-8-yl)acrylamide
  • TAS-6417;TAS 6417;TAS6417
  • TAS6417

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