WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 207108
Description: TAS6417, also known as CLN-081, is a Novel EGFR Inhibitor Targeting Exon 20 Insertion Mutations. TAS6417 inhibited EGFR with various exon 20 insertion mutations more potently than it inhibited the WT. TAS6417 inhibited EGFR phosphorylation and downstream molecules in NSCLC cell lines expressing EGFR exon 20 insertions, resulting in caspase activation. These characteristics led to marked tumor regression in vivo in both a genetically engineered model and in a patient-derived xenograft model. Furthermore, TAS6417 provided a survival benefit with good tolerability in a lung orthotopic implantation mouse model.
MedKoo Cat#: 207108
Chemical Formula: C23H20N6O
Exact Mass: 396.1699
Molecular Weight: 396.454
Elemental Analysis: C, 69.68; H, 5.09; N, 21.20; O, 4.04
Synonym: TAS6417; TAS-6417; TAS 6417; CLN-081; CLN081; CLN081;
IUPAC/Chemical Name: (S)-N-(4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dihydropyrimido[5,4-b]indolizin-8-yl)acrylamide
InChi Key: MKCYPWYURWOKST-INIZCTEOSA-N
InChi Code: InChI=1S/C23H20N6O/c1-3-18(30)28-16-8-13(2)21-19(15-9-14-6-4-5-7-17(14)25-10-15)20-22(24)26-12-27-23(20)29(21)11-16/h3-10,12,16H,1,11H2,2H3,(H,28,30)(H2,24,26,27)/t16-/m0/s1
SMILES Code: NC1=C2C(N3C(C(C)=C[C@@H](C3)NC(C=C)=O)=C2C4=CC5=CC=CC=C5N=C4)=NC=N1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 396.454 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Hasako S, Terasaka M, Abe N, Uno T, Ohsawa H, Hashimoto A, Fujita R, Tanaka K,
Okayama T, Wadhwa R, Miyadera K, Aoyagi Y, Yonekura K, Matsuo K. 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. Epub 2018 May 10. PubMed