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TAS6417 - 99%, high purity , Epidermal growth factor receptor erbB1 inhibitor, CAS No.1661854-97-2, Epidermal growth factor receptor erbB1 inhibitor

COA

Grade & Purity:

Moligand™

≥99%

Cas Number: 1661854-97-2
Molecular Weight: 396.44
PubChem CID: 117918742
PubChem SID: 504772840

In stock

Item Number

T414199

Grouped product items
SKU	Size	Availability	Price
T414199-1mg	1mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$84.90
T414199-5mg	5mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$296.90
T414199-10mg	10mg	3	$494.90
T414199-25mg	25mg	2	$1,038.90
T414199-50mg	50mg	2	$1,484.90
T414199-100mg	100mg	1	$2,375.90

EGFR/ErbB1 Selective Inhibitors | Activators

View related series

Apoptosis (4276) EGFR (254) epidermal growth factor receptor Inhibitor (73) JAK/STAT Signaling (507) Protein Tyrosine Kinase/RTK (1314) Receptor Tyrosine Kinase (1260)

Basic Description

Synonyms	1661854-97-2 \| AS-79368 \| D93895 \| 2-Propenamide, N-((8S)-4-amino-8,9-dihydro-6-methyl-5-(3-quinolinyl)pyrimido(5,4-b)indolizin-8-yl)- \| tert-butoxycarbonylamino-(dimethoxy-phosphoryl)-acetic acid methyl ester \| AKOS040742682 \| CLN-081 \| MKCYPWYURWOKST-IN
Specifications & Purity	Moligand™, ≥99%
Biochemical and Physiological Mechanisms	TAS6417 (CLN-081, TPC-064) is a novel EGFR inhibitor that targets EGFR exon 20 insertion mutations while sparing wild-type (WT) EGFR. IC50 values ranges from 1.1 ± 0.1 to 8.0 ± 1.1 nmol/L.
Storage Temp	Protected from light,Store at -20°C,Argon charged
Shipped In	Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available.
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Epidermal growth factor receptor erbB1 inhibitor
Product Description	Information TAS6417 (CLN-081, TPC-064) is a novelEGFRinhibitor that targets EGFR exon 20 insertion mutations while sparing wild-type (WT) EGFR. IC50 values ranges from 1.1 ± 0.1 to 8.0 ± 1.1 nmol/L. Targets EGFR(d746-750/T790M) (Cell-free assay); TXK (Cell-free assay); EGFR(d746-750) (Cell-free assay); EGFR L858R (Cell-free assay); EGFR T790M/L858R (Cell-free assay) 31954,1.1 nM; 1.1 nM; 1.4 nM; 1.9 nM; 2 nM In vitro Of the 255 kinases tested, TAS6417 inhibits 25 kinases other than EGFR with IC50 values less than 1,000 nmol/L, which was 100 times higher than its IC50 value against WT EGFR. It inhibits only six kinases containing TXK, BMX, HER4, TEC, BTK, and JAK3, with IC50 values less than 10 times that against WT EGFR. TAS6417 inhibits proliferation of Ba/F3 cells driven by various EGFR exon 20 insertion mutations, with IC50 values ranging from 5.05 ± 1.33 nmol/L to 150 ± 53 nmol/L. It also suppresses the growth of cells expressing exon 20 insertion mutations of the EGFR gene, with a GI50 value of 86.5 ± 28.5 nmol/L for LXF 2478L cells and 45.4 ± 2.6 nmol/L for NCI-H1975 EGFR D770_N771insSVD cells. TAS6417 has no effect on EGFR-independent proliferation in NCI-H23 or NCI-H460 cells. In vivo TAS6417 causes persistent tumor regression in vivo in EGFR exon 20 insertion-driven tumor models. The tumor regression occurrs quickly after TAS6417 treatment and persists during the treatment period. Pharmacokinetic analysis reveals that the plasma concentration of TAS6417, administered at 50 and 100 mg/kg to mice, decreases rapidly in the first 4 hours. In contrast, although the effective doses in the rat model exhibit lower maximum plasma concentration (Cmax) values than those in the mouse model, the plasma concentrations tend to be more persistent, lasting up to 8 hours. TAS6417 inhibits mutant EGFR in tumors but not WT EGFR in skin tissues. It prolongs survival of animals bearing lung cancer. Cell Research(from reference) Cell lines：LXF 2478L cells and NCI-H1975 EGFR D770_N771insSVD cells Concentrations：0-1 μM Incubation Time：6 and 24 hours

Product Properties

ALogP	3.124
HBD Count	2
Rotatable Bond	3

Associated Targets(Human)

EGFR Tclin Epidermal growth factor receptor (0 Activities)

Discover Target: EGFR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Mechanisms of Action

Mechanism of Action	Action Type	target ID	Target Name	Target Type	Target Organism	Binding Site Name	References

Names and Identifiers

Pubchem Sid	504772840
Pubchem Sid Url	https://pubchem.ncbi.nlm.nih.gov/substance/504772840
IUPAC Name	N-[(8S)-4-amino-6-methyl-5-quinolin-3-yl-8,9-dihydropyrimido[5,4-b]indolizin-8-yl]prop-2-enamide
INCHI	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
InChIKey	MKCYPWYURWOKST-INIZCTEOSA-N
Smiles	CC1=CC(CN2C1=C(C3=C(N=CN=C32)N)C4=CC5=CC=CC=C5N=C4)NC(=O)C=C
Isomeric SMILES	CC1=C[C@@H](CN2C1=C(C3=C(N=CN=C32)N)C4=CC5=CC=CC=C5N=C4)NC(=O)C=C
PubChem CID	117918742
Molecular Weight	396.44

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

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4 results found

Lot Number	Certificate Type	Date	Item
G2221231	Certificate of Analysis	May 09, 2025	T414199
G2221230	Certificate of Analysis	May 09, 2025	T414199
G2221229	Certificate of Analysis	May 09, 2025	T414199
G2221232	Certificate of Analysis	May 09, 2025	T414199

Chemical and Physical Properties

Solubility	Solubility (25°C) In vitro DMSO: 79 mg/mL (199.27 mM); Ethanol: 79 mg/mL (199.27 mM); Water: Insoluble;
Sensitivity	Light sensitive
DMSO(mg / mL) Max Solubility	79
DMSO(mM) Max Solubility	199.273534456664
Water(mg / mL) Max Solubility	＜1
Molecular Weight	396.400 g/mol
XLogP3	2.300
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	5
Rotatable Bond Count	3
Exact Mass	396.17 Da
Monoisotopic Mass	396.17 Da
Topological Polar Surface Area	98.700 Å²
Heavy Atom Count	30
Formal Charge	0
Complexity	710.000
Isotope Atom Count	0
Defined Atom Stereocenter Count	1
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
The total count of all stereochemical bonds	0
Covalently-Bonded Unit Count	1

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