Referencia número: HY-15375

Allitinib

(Synonyms: AST-1306; ALS 1306)

3 Cited Publications

Revisión del cliente

Based on 3 publication(s) in Google Scholar

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.

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Pureza: 98.88%
No. CAS: 897383-62-9
Fòrmula: C₂₄H₁₈ClFN₄O₂
Peso molecular:448.88

Almacenamiento:

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)

Allitinib Chemical Structure

No. CAS: 897383-62-9

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

EGFR

0.5 nM (IC₅₀)

EGFR^L858R/T790M

12 nM (IC₅₀)

ErbB2

3 nM (IC₅₀)

ErbB4

0.8 nM (IC₅₀)

Ver todos los productos específicos de isoformas EGFR :

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	6.2 μM Compound: Chemical Probe: AST1306	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by SRB assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 21789172]
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]
BT-474	IC₅₀	0.97 μM Compound: Chemical Probe: AST1306	Antiproliferative activity against human BT-474 cells assessed as reduction in cell viability after 72 hrs by SRB assay Antiproliferative activity against human BT-474 cells assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 21789172]
Calu-3	IC₅₀	0.23 μM Compound: Chemical Probe: AST1306	Antiproliferative activity against human Calu-3 cells assessed as reduction in cell viability after 72 hrs by SRB assay Antiproliferative activity against human Calu-3 cells assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 21789172]
MCF7	IC₅₀	16 μM Compound: Chemical Probe: AST1306	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by SRB assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 21789172]
MDA-MB-468	IC₅₀	6.2 μM Compound: Chemical Probe: AST1306	Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability after 72 hrs by SRB assay Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 21789172]
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]
NCI-H23	IC₅₀	6.2 μM Compound: Chemical Probe: AST1306	Antiproliferative activity against human NCI-H23 cells assessed as reduction in cell viability after 72 hrs by SRB assay Antiproliferative activity against human NCI-H23 cells assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 21789172]
SK-OV-3	IC₅₀	6.2 μM Compound: Chemical Probe: AST1306	Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell viability after 72 hrs by SRB assay Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 21789172]

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.

Chemical Information

No. CAS 897383-62-9
Appearance Solid
Peso molecular 448.88
Fòrmula C₂₄H₁₈ClFN₄O₂
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
Synonyms

AST-1306; ALS 1306
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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)

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

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (222.78 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)

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

2.2278 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

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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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 90% Corn Oil

Solubility: 2.5 mg/mL (5.57 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 2

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.

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (277 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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)
Instrucciones de manejo (2659 KB)

Referencias

[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	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
	50 mM	0.0446 mL	0.2228 mL	0.4456 mL	1.1139 mL
	60 mM	0.0371 mL	0.1856 mL	0.3713 mL	0.9282 mL
	80 mM	0.0278 mL	0.1392 mL	0.2785 mL	0.6962 mL
	100 mM	0.0223 mL	0.1114 mL	0.2228 mL	0.5569 mL

Keywords

Allitinib

3 Cited Publications

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Allitinib

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

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Bioactive Compound Library

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Publications Citing Use of MedChemExpress (MCE) Allitinib

Ver todos los productos específicos de isoformas EGFR

Actividad biológica

Chemical Information

Publications (3)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Allitinib Related Classifications

HY-15375 Related Classifications