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MedKoo CAT#: 207108

CAS#: 1661854-97-2

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.

Chemical Structure

CAS# 1661854-97-2

Theoretical Analysis

MedKoo Cat#: 207108
Name: TAS6417
CAS#: 1661854-97-2
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

Price and Availability

Size Price Availability Quantity
25.0mg USD 250.0 2 Weeks
50.0mg USD 450.0 2 Weeks
100.0mg USD 750.0 2 Weeks
200.0mg USD 1250.0 2 Weeks
500.0mg USD 2650.0 2 Weeks
1.0g USD 3850.0 2 Weeks
2.0g USD 6450.0 2 Weeks
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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 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

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 20.0 50.44

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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

Molarity Calculator

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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
PMID: 29748209.


25.0mg / USD 250.0