Cat. No.: HY-13427

Allitinib tosylate

(Synonyms: AST-1306 (TsOH))

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

Allitinib tosylate (AST-1306 (TsOH)) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC₅₀s of 0.5 and 3 nM, respectively. Allitinib tosylate also inhibits ErbB4 with an IC₅₀ of 0.8 nM. Allitinib tosylate is an anilino-quinazoline compound and has anti-cancer activity

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Pureté: 99.54%
CAS No.: 1050500-29-2
Formule: C₃₁H₂₆ClFN₄O₅S
Masse moléculaire:621.08

Stockage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Allitinib tosylate Chemical Structure

CAS No.: 1050500-29-2

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

Activité biologique

Description

IC₅₀ & Target^[1]

EGFR

0.5 nM (IC₅₀)

ErbB2

3 nM (IC₅₀)

EGFR^L858R/T790M

12 nM (IC₅₀)

ErbB4

0.8 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform EGFR :

In Vitro

AST1306 tosylate (AST-1306 (TsOH); 0.19-6.25 μM; 72 hours) induces a significant, concentration-dependent inhibition of the growth of HIH3T3-EGFR T790M/L858R cells^[1].
AST1306 tosylate inhibits the activation of tyrosine kinases and downstream signaling pathways in A549 cells, Calu-3 cells and SK-OV-3 cells. AST1306 tosylate dose-dependently and markedly inhibits EGF-induced EGFR phosphorylation in A549 cells^[1].
AST1306 tosylate (0.1, 0.5, 1.0, 5.0 μM) can dramatically inhibit the growth of both tumor cells on soft agar, and SK-OV-3 cells exhibited much more sensitivity than that of A549 cells^[1].
AST1306 tosylate (0.001-1.0 μM; 4 hours) is more than 3000-fold selective for ErbB family kinases over other kinase families^[1].
AST1306 tosylate potently inhibits the EGFR T790M/L858R double mutant, exhibiting an IC₅₀ value of 12±2 nmol/L^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

NIH3T3 parental cells and NIH3T3 cells
Concentration:

0.19, 0.39, 0.78, 1.56, 3.13, 6.25 μM
Incubation Time:

72 hours
Result:

Induced a significant, concentration-dependent inhibition of the growth of HIH3T3-EGFR T790M/L858R cells.

Western Blot Analysis^[1]

Cell Line:

A549 cells , Calu-3 cells and SK-OV-3 cells
Concentration:

0.001, 0.01, 0.1, 1.0 μM
Incubation Time:

4 hours
Result:

Inhibits the activation of tyrosine kinases and downstream signaling pathways.

In Vivo

AST1306 tosylate (AST-1306 (TsOH); p.o.; 25-100 mg/kg; twice daily; for 28 days) causes a dramatic suppression of tumor growth in SK-OV-3 and Calu-3 xenograft models^[1].

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

Animal Model:

Nude mice with SK-OV-3 and Calu-3 tumors^[1]
Dosage:

25, 50, 100 mg/kg
Administration:

p.o.; twice daily; for 28 days
Result:

Caused a dramatic suppression of tumor growth.

Chemical Information

CAS No. 1050500-29-2
Appearance Solid
Masse moléculaire 621.08
Formule C₃₁H₂₆ClFN₄O₅S
Color Light yellow to yellow
SMILES

FC1=CC=CC(COC2=C(Cl)C=C(NC3=NC=NC4=C3C=C(NC(C=C)=O)C=C4)C=C2)=C1.O=S(C5=CC=C(C)C=C5)(O)=O
Synonyms

AST-1306 (TsOH)
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (3)

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Journal Impact Factor

Sci Adv

Tissue-specific inflammation induces cell state plasticity with oncogenic addiction in mucosal melanoma. [Abstract]

2026 Apr 3;12(14):eady4536. PMID: 41920996
Cell Rep

Carvedilol sensitizes chemotherapy by targeting STING to boost anti-tumor immunity. [Abstract]

2025 Apr 16;44(5):115572. PMID: 40249703
Sci Data

High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]

2024 Sep 19;11(1):1024. PMID: 39300112

Solvant et solubilité

In Vitro:

DMSO : 50 mg/mL (80.50 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

1.6101 mL

8.0505 mL

16.1010 mL

5 mM

0.3220 mL

1.6101 mL

3.2202 mL

10 mM

0.1610 mL

0.8050 mL

1.6101 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 (sealed storage, away from moisture). 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: ≥ 2.5 mg/mL (4.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

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 (281 KB)
SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 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]. Xie H, Lin L, Tong L et al. AST1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo. PLoS One. 2011;6(7):e21487. [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	1.6101 mL	8.0505 mL	16.1010 mL	40.2525 mL
	5 mM	0.3220 mL	1.6101 mL	3.2202 mL	8.0505 mL
	10 mM	0.1610 mL	0.8050 mL	1.6101 mL	4.0252 mL
	15 mM	0.1073 mL	0.5367 mL	1.0734 mL	2.6835 mL
	20 mM	0.0805 mL	0.4025 mL	0.8050 mL	2.0126 mL
	25 mM	0.0644 mL	0.3220 mL	0.6440 mL	1.6101 mL
	30 mM	0.0537 mL	0.2683 mL	0.5367 mL	1.3417 mL
	40 mM	0.0403 mL	0.2013 mL	0.4025 mL	1.0063 mL
	50 mM	0.0322 mL	0.1610 mL	0.3220 mL	0.8050 mL
	60 mM	0.0268 mL	0.1342 mL	0.2683 mL	0.6709 mL
	80 mM	0.0201 mL	0.1006 mL	0.2013 mL	0.5032 mL

Keywords

Allitinib tosylate

3 Cited Publications

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Allitinib tosylate

Immunology/Inflammation Compound Library

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Publications Citing Use of MedChemExpress (MCE) Allitinib tosylate

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

Allitinib tosylate Related Classifications

HY-13427 Related Classifications