Cat. No.: HY-112299

Zipalertinib

(Synonyms: TAS6417; CLN-081)

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

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.

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Pureté: 99.62%
CAS No.: 1661854-97-2
Formule: C₂₃H₂₀N₆O
Masse moléculaire:396.44

Stockage:

4°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Zipalertinib Chemical Structure

CAS No.: 1661854-97-2

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (3)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

EGFR

1.1-8.0 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform EGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	5 nM Compound: CLN-081; TAS6417	Antiproliferative activity against mouse Ba/F3 cells harboring EGFR-D770-N771ins_G mutant incubated for 3 days by Cell Titer-Glo assay Antiproliferative activity against mouse Ba/F3 cells harboring EGFR-D770-N771ins_G mutant incubated for 3 days by Cell Titer-Glo assay	[PMID: 37669428]
BaF3	IC₅₀	5 nM Compound: CLN-081; TAS6417	Antiproliferative activity against mouse Ba/F3 cells harboring EGFR-H773-V774ins_PH mutant incubated for 3 days by Cell Titer-Glo assay Antiproliferative activity against mouse Ba/F3 cells harboring EGFR-H773-V774ins_PH mutant incubated for 3 days by Cell Titer-Glo assay	[PMID: 37669428]
BaF3	IC₅₀	676 nM Compound: CLN-081; TAS6417	Antiproliferative activity against mouse BaF3 cells harboring wild type EGFR incubated for 3 days by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells harboring wild type EGFR incubated for 3 days by Cell Titer-Glo assay	[PMID: 37669428]
NIH3T3	IC₅₀	<4.48 nM Compound: CLN-081; TAS6417	Antiproliferative activity against mouse NIH/3T3 cells harboring EGFR-A763_Y764insFQEA incubated for 72 hrs by Cell Titer-Glo assay Antiproliferative activity against mouse NIH/3T3 cells harboring EGFR-A763_Y764insFQEA incubated for 72 hrs by Cell Titer-Glo assay	[PMID: 37669428]
NIH3T3	IC₅₀	23.4 nM Compound: CLN-081; TAS6417	Antiproliferative activity against mouse NIH/3T3 cells harboring EGFR-D770-N771ins_SVD incubated for 72 hrs by Cell Titer-Glo assay Antiproliferative activity against mouse NIH/3T3 cells harboring EGFR-D770-N771ins_SVD incubated for 72 hrs by Cell Titer-Glo assay	[PMID: 37669428]
NIH3T3	IC₅₀	368 nM Compound: CLN-081; TAS6417	Antiproliferative activity against mouse NIH/3T3 cells harboring wild type EGFR incubated for 72 hrs by Cell Titer-Glo assay Antiproliferative activity against mouse NIH/3T3 cells harboring wild type EGFR incubated for 72 hrs by Cell Titer-Glo assay	[PMID: 37669428]
NIH3T3	IC₅₀	66.7 nM Compound: CLN-081; TAS6417	Antiproliferative activity against mouse NIH/3T3 cells harboring EGFR-H773-V774ins_NPH incubated for 72 hrs by Cell Titer-Glo assay Antiproliferative activity against mouse NIH/3T3 cells harboring EGFR-H773-V774ins_NPH incubated for 72 hrs by Cell Titer-Glo assay	[PMID: 37669428]
NIH3T3	IC₅₀	78.2 nM Compound: CLN-081; TAS6417	Antiproliferative activity against mouse NIH/3T3 cells harboring EGFR-V769_D770insASV incubated for 72 hrs by Cell Titer-Glo assay Antiproliferative activity against mouse NIH/3T3 cells harboring EGFR-V769_D770insASV incubated for 72 hrs by Cell Titer-Glo assay	[PMID: 37669428]

In Vitro

Zipalertinib (TAS6417) inhibits EGFR phosphorylation and downstream molecules in NSCLC cell lines expressing EGFR exon 20 insertions, resulting in caspase activation^[1].
? Zipalertinib (TAS6417) is a robust inhibitor against the most common EGFR mutations (exon 19 deletions and L858R) and the most potent against cells harboring EGFR-T790M (1st/2nd generation TKI resistance mutation)^[2].
? Zipalertinib (TAS6417) covalently modified the cysteine residue at position 797 of recombinant EGFR harboring an in-frame insertion mutation in the exon 20 region^[1].
? Zipalertinib (TAS6417) inhibits EGFR signal transduction, leading to cell growth inhibition and apoptosis induction in NSCLC cells driven by EGFR exon 20 insertion mutations^[1].
? Zipalertinib (TAS6417) (0-10 μM) inhibits cell proliferation and EGFR signaling in NSCLC cell lines harboring EGFR common mutations in the presence or absence of T790M^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis^[2]

Cell Line:

PC-9, H1975, BID007, BID019, BEAS-2B cells.
Concentration:

0-10 μM.
Incubation Time:

24-48 h.
Result:

Led to apoptosis via inhibition of mutant EGFR.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1661854-97-2
Appearance Solid
Masse moléculaire 396.44
Formule C₂₃H₂₀N₆O
Color White to yellow
SMILES

NC1=C2C(N3C(C(C)=C[C@@H](C3)NC(C=C)=O)=C2C4=CC5=CC=CC=C5N=C4)=NC=N1
Synonyms

TAS6417; CLN-081
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Publications (3)

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Clin Cancer Res

STX-721, a Covalent EGFR/HER2 Exon 20 Inhibitor, Utilizes Exon 20-Mutant Dynamic Protein States and Achieves Unique Mutant Selectivity Across Human Cancer Models. [Abstract]

2025 Jun 4:OF1-OF17. PMID: 40465424
Lung Cancer

Efficacy of EGFR tyrosine kinase inhibitors in patients with non-small cell lung cancer with EGFR exon 19 insertions: clinical-genomic, preclinical analysis through LC-SCRUM-Asia (multi-institutional genomic screening registry). [Abstract]

2025 Apr:202:108479. PMID: 40088581
JTO Clin Res Rep

The Impact of On-Target Resistance Mediated by EGFR-T790M or EGFR-C797S on EGFR Exon 20 Insertion Mutation Active Tyrosine Kinase Inhibitors. [Abstract]

2023 Nov 27;5(1):100614. PMID: 38229766

Solvant et solubilité

In Vitro:

DMSO : 125 mg/mL (315.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5224 mL

12.6122 mL

25.2245 mL

5 mM

0.5045 mL

2.5224 mL

5.0449 mL

10 mM

0.2522 mL

1.2612 mL

2.5224 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (5.25 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.25 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (286 KB)
SDS (252 KB)
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- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
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- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Hasako S, et al. TAS6417, A Novel EGFR Inhibitor Targeting Exon 20 Insertion Mutations. Mol Cancer Ther. 2018 Aug;17(8):1648-1658. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5224 mL	12.6122 mL	25.2245 mL	63.0612 mL
	5 mM	0.5045 mL	2.5224 mL	5.0449 mL	12.6122 mL
	10 mM	0.2522 mL	1.2612 mL	2.5224 mL	6.3061 mL
	15 mM	0.1682 mL	0.8408 mL	1.6816 mL	4.2041 mL
	20 mM	0.1261 mL	0.6306 mL	1.2612 mL	3.1531 mL
	25 mM	0.1009 mL	0.5045 mL	1.0090 mL	2.5224 mL
	30 mM	0.0841 mL	0.4204 mL	0.8408 mL	2.1020 mL
	40 mM	0.0631 mL	0.3153 mL	0.6306 mL	1.5765 mL
	50 mM	0.0504 mL	0.2522 mL	0.5045 mL	1.2612 mL
	60 mM	0.0420 mL	0.2102 mL	0.4204 mL	1.0510 mL
	80 mM	0.0315 mL	0.1577 mL	0.3153 mL	0.7883 mL
	100 mM	0.0252 mL	0.1261 mL	0.2522 mL	0.6306 mL

Zipalertinib

3 Cited Publications

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Zipalertinib

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Publications Citing Use of MedChemExpress (MCE) Zipalertinib

Voir tous les produits spécifiques à Isoform EGFR

Activité biologique

Chemical Information

Publications (3)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Zipalertinib Related Classifications

HY-112299 Related Classifications