Fig. 1 · Structure

Documents & Downloads

AST-1306

Cat. No. A11155 CAS 897383-62-9

EGFR Inhibitor

AST-1306, a novel anilino-quinazoline compound, inhibits the enzymatic activities of wild-type epidermal growth factor receptor (EGFR) and ErbB2 as well as EGFR resistant mutant in both cell-free and cell-based systems.

In Stock

Free Aliquoting for Your Order

Tell us your preferred amount per vial. We’ll confirm the options.

Biological Activity

Target & Activity

Target Activity Value
EGFR IC50 0.5 nM
ErbB2 IC50 3 nM
EGFR(L858R)/T790M IC50 12 nM
ErbB4 IC50 0.8 nM

Cellular Effect

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

In Vitro Studies

The tested compound was evaluated in an EGFR cell-free assay for tyrosine kinase activities. A quantitative activity result was reported. SCC25 cells received compound treatment for 72 hours, with DMSO-treated cells as the control. The reported cell viability value was 207.29 ± 11.6 nM. NCI-H1975 cells received compound treatment, and cell viability was assessed 72 h after drug treatments using DMSO control values. The reported result was 0.21 ± 0.09 µM. In an ErbB2 cell-free assay, the study compound yielded a tyrosine kinase activity result of 3.0±1.5 nmol/L. [1,2,3]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Tyrosine Kinase Activities in a Cell-Free Assay

Cell-based study · EGFR [1]

The tested compound was evaluated in an EGFR cell-free assay for tyrosine kinase activities. A quantitative activity result was reported.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
tyrosine kinase activitiesIC50 0.5±0.2 nmol/L[1]

Literature-Reported Treatment Conditions

Method
cell-free assay
Reported limits
Not stated in the sentences used: dose, schedule, vehicle, control.
Methods and source locations

Compound reported in the paper: AST-1306

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Materials and Methods > Cell proliferation, tyrosine kinase, and Western blot assay (S7); Results > AST1306 selectively inhibits the tyrosine kinase activities of EGFR and ErbB2 in vitro (S46, S47); Table 1 (T1.h1, T1.r1)

tyrosine kinase activities: tyrosine kinase activities — Materials and Methods > Cell proliferation, tyrosine kinase, and Western blot assay (S7); Table 1 (T1.h1, T1.r1)

Compound treatment and cell viability in SCC25 cells

Cell-based study · SCC25 [2]

SCC25 cells received compound treatment for 72 hours, with DMSO-treated cells as the control. The reported cell viability value was 207.29 ± 11.6 nM.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Cell viabilityIC50 207.29 ± 11.6 nM[2]

Literature-Reported Treatment Conditions

Treatment concentration
100, 200, 400, 600, 800 and 1000 nM
Exposure duration
72 hours
Method
in DMEM-0.5%
Vehicle
DMSO
Methods and source locations

Compound reported in the paper: AST-1306; Compound label in the paper: Allitinib

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

RESULTS > Viability effect of cetuximab, afatinib and allitinib in hnscc cell lines (S13); MATERIALS AND METHODS > Pharmacological agents (S62, S63); MATERIALS AND METHODS > Cell viability (S64, S66, S68)

Cell viability: Cell viability; comparator: DMSO treated control cells — RESULTS > Viability effect of cetuximab, afatinib and allitinib in hnscc cell lines (S13); MATERIALS AND METHODS > Cell viability (S64)

Cell viability after drug treatment in NCI-H1975 cells

Cell-based study · NCI-H1975 [3]

NCI-H1975 cells received compound treatment, and cell viability was assessed 72 h after drug treatments using DMSO control values. The reported result was 0.21 ± 0.09 µM.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
cell viabilityIC50 0.21 ± 0.09 µM[3]

Literature-Reported Treatment Conditions

Treatment concentration
0.2; 0.4; 0.6; 0.8; 1.0; 2.0; 5.0 μM
Exposure duration
72 h after drug treatments
Vehicle
DMSO
Reported limits
Not stated in the sentences used: route.
Methods and source locations

Compound reported in the paper: AST-1306; Compound label in the paper: Allitinib

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

4. Materials and Methods > 4.2. Pharmacological Agents (S61); 4. Materials and Methods > 4.3. Cytotoxicity, Growth Inhibition, and Proliferation Analyses (S64, S66, S68); Table 1 (T1.h1, T1.h2, T1.r1)

cell viability: cell viability; comparator: DMSO control values — 4. Materials and Methods > 4.3. Cytotoxicity, Growth Inhibition, and Proliferation Analyses (S64); Table 1 (T1.h1, T1.h2, T1.r1)

ErbB2 Activity in a Cell-Free Assay

Cell-based study · ErbB2 [1]

In an ErbB2 cell-free assay, the study compound yielded a tyrosine kinase activity result of 3.0±1.5 nmol/L.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
tyrosine kinase activitiesIC50 3.0±1.5 nmol/L[1]

Literature-Reported Treatment Conditions

Method
cell-free assay
Reported limits
Not stated in the sentences used: dose, schedule, vehicle, control.
Methods and source locations

Compound reported in the paper: AST-1306

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Materials and Methods > Cell proliferation, tyrosine kinase, and Western blot assay (S7); Results > AST1306 selectively inhibits the tyrosine kinase activities of EGFR and ErbB2 in vitro (S46, S47); Table 1 (T1.h1, T1.r2)

tyrosine kinase activities: tyrosine kinase activities — Materials and Methods > Cell proliferation, tyrosine kinase, and Western blot assay (S7); Table 1 (T1.h1, T1.r2)

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 897383-62-9
Applications EGFR Inhibitor
Formula C24H18ClFN4O2
Molecular Weight 448.9
SMILES
C=CC(=O)NC1=CC2=C(C=C1)N=CN=C2NC3=CC(=C(C=C3)OCC4=CC(=CC=C4)F)Cl

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [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). PMID: 21789172 DOI: 10.1371/journal.pone.0021487 Source material
  2. [2] Silva-Oliveira RJ, Melendez M, Martinho O, et al. AKT can modulate the in vitro response of HNSCC cells to irreversible EGFR inhibitors. Oncotarget (2017). PMID: 28881811 DOI: 10.18632/oncotarget.18395 Source material
  3. [3] da Silva-Oliveira RJ, Gomes INF, da Silva LS, et al. Efficacy of Combined Use of Everolimus and Second-Generation Pan-EGRF Inhibitors in KRAS Mutant Non-Small Cell Lung Cancer Cell Lines. Int J Mol Sci (2022). PMID: 35887120 DOI: 10.3390/ijms23147774 Source material

Added to your cart

View Cart Checkout
Loading...