Allitinib (Synonyms: AST-1306; ALS 1306)

Name: Allitinib
Brand: MedChemExpress
SKU: HY-15375
Rating: 4.5 (1 reviews)

Cat. No.: HY-15375 Purity: 99.36%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

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

Allitinib Chemical Structure

CAS No. : 897383-62-9

Size	Price	Stock	Quantity
5 mg	USD 140	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 225	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 630	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 890	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Allitinib:

Allitinib tosylate In-stock

1 Publications Citing Use of MCE Allitinib

•Sci Data. 2024 Sep 19.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All EGFR Isoform Specific Products:

View All Isoforms

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

EGFR

0.5 nM (IC₅₀)

EGFR^L858R/T790M

12 nM (IC₅₀)

ErbB2

3 nM (IC₅₀)

ErbB4

0.8 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	0.2 μM Compound: AST1306	Antiproliferative activity against human A431 cells over-expressing EGFR gene after 72 hrs by SRB assay Antiproliferative activity against human A431 cells over-expressing EGFR gene after 72 hrs by SRB assay	[PMID: 22227214]
A549	IC₅₀	6.8 μM Compound: AST1306	Antiproliferative activity against human A549 cells over-expressing EGFR gene after 72 hrs by SRB assay Antiproliferative activity against human A549 cells over-expressing EGFR gene after 72 hrs by SRB assay	[PMID: 22227214]
NCI-H1975	IC₅₀	0.7 μM Compound: AST1306	Antiproliferative activity against human NCI-H1975 cells over-expressing EGFR mutant gene after 72 hrs by SRB assay Antiproliferative activity against human NCI-H1975 cells over-expressing EGFR mutant gene after 72 hrs by SRB assay	[PMID: 22227214]

In Vitro

AST1306 (AST-1306; 0.19-6.25 μM; 72 hours) induces a significant, concentration-dependent inhibition of the growth of HIH3T3-EGFR T790M/L858R cells^[1].
AST1306 inhibits the activation of tyrosine kinases and downstream signaling pathways in A549 cells, Calu-3 cells and SK-OV-3 cells. AST1306 dose-dependently and markedly inhibits EGF-induced EGFR phosphorylation in A549 cells^[1].
AST1306 (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 (0.001-1.0 μM; 4 hours) is more than 3000-fold selective for ErbB family kinases over other kinase families^[1].
AST1306 potently inhibits the EGFR T790M/L858R double mutant, exhibiting an IC₅₀ value of 12 nM^[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 (AST-1306; 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

448.88

Formula

C₂₄H₁₈ClFN₄O₂

CAS No.

897383-62-9

Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

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

Solvent & Solubility

In Vitro:

DMSO : 20 mg/mL (44.56 mM; ultrasonic and warming and heat to 60°C; 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	2.2278 mL	11.1388 mL	22.2777 mL
5 mM	0.4456 mL	2.2278 mL	4.4555 mL
10 mM	0.2228 mL	1.1139 mL	2.2278 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 and light). 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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 mg/mL (4.46 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 and light)

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: 99.36%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (248 KB) HNMR (138 KB) LCMS (90 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	2.2278 mL	11.1388 mL	22.2777 mL	55.6942 mL
	5 mM	0.4456 mL	2.2278 mL	4.4555 mL	11.1388 mL
	10 mM	0.2228 mL	1.1139 mL	2.2278 mL	5.5694 mL
	15 mM	0.1485 mL	0.7426 mL	1.4852 mL	3.7129 mL
	20 mM	0.1114 mL	0.5569 mL	1.1139 mL	2.7847 mL
	25 mM	0.0891 mL	0.4456 mL	0.8911 mL	2.2278 mL
	30 mM	0.0743 mL	0.3713 mL	0.7426 mL	1.8565 mL
	40 mM	0.0557 mL	0.2785 mL	0.5569 mL	1.3924 mL

Allitinib 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:

Allitinib897383-62-9AST-1306 ALS 1306AST1306AST 1306ALS1306ALS 1306ALS-1306EGFREpidermal growth factor receptorErbB-1HER1Irreversibleanilino-quinazolineanti-cancerInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Allitinib (Synonyms: AST-1306; ALS 1306)

Customer Review

Other Forms of Allitinib:

Allitinib Related Antibodies

1 Publications Citing Use of MCE Allitinib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All EGFR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Allitinib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Allitinib Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report