Allitinib tosylate (Synonyms: AST-1306 (TsOH))

Name: Allitinib tosylate
Brand: MedChemExpress
SKU: HY-13427
Rating: 4.5 (1 reviews)

Cat. No.: HY-13427 Purity: 99.83%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

For research use only. We do not sell to patients.

Allitinib tosylate Chemical Structure

CAS No. : 1050500-29-2

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 205	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 205	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1250	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Allitinib tosylate:

Allitinib Get quote

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

EGFR

0.5 nM (IC₅₀)

ErbB2

3 nM (IC₅₀)

EGFR^L858R/T790M

12 nM (IC₅₀)

ErbB4

0.8 nM (IC₅₀)

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.

Clinical Trial

Molecular Weight

621.08

Formula

C₃₁H₂₆ClFN₄O₅S

CAS No.

1050500-29-2

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.83%

Select Batch:

Data Sheet (278 KB) SDS (252 KB)

COA (253 KB) LCMS (266 KB)

Handling Instructions (2659 KB)

References

[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]

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

Allitinib tosylate Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Allitinib1050500-29-2AST-1306 (TsOH)EGFREpidermal growth factor receptorErbB-1HER1Irreversibleanilino-quinazolineanti-cancerInhibitorinhibitorinhibit

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Allitinib tosylate (Synonyms: AST-1306 (TsOH))

Customer Review

Other Forms of Allitinib tosylate:

Allitinib tosylate Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All EGFR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Allitinib tosylate Related Antibodies

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Complete Stock Solution Preparation Table

Allitinib tosylate Related Classifications

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