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Cat. No.: HY-144766

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ATX inhibitor 13

ATX inhibitor 13 (10c) is an orally active and potent ATX inhibitor, with an IC₅₀ of 3.4 nM. ATX inhibitor 13 inhibits proliferation and migration, and induces apoptosis and G2 phase arrest in RAW264.7 cells. ATX inhibitor 13 suppresses tumor cell colony formation.

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

CAS No.: 2485779-34-6
Formula: C₃₁H₃₅Cl₂N₅O₃
Molecular Weight:596.55

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

ATX inhibitor 13 Chemical Structure

CAS No.: 2485779-34-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

ATX

3.4 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	6.59 μM Compound: 10c	Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35436669]
Hep 3B2	IC₅₀	0.58 μM Compound: 10c	Cytotoxicity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35436669]
MCF7	IC₅₀	3.87 μM Compound: 10c	Cytotoxicity against human MCF-7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human MCF-7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35436669]
MDA-MB-231	IC₅₀	3.29 μM Compound: 10c	Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35436669]
NCI-H1581	IC₅₀	4.76 μM Compound: 10c	Cytotoxicity against human NCI-H1581 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human NCI-H1581 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35436669]
NCI-H2228	IC₅₀	4.27 μM Compound: 10c	Cytotoxicity against human H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35436669]
RAW264.7	IC₅₀	0.63 μM Compound: 10c	Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35436669]

In Vitro

ATX inhibitor 13 (compound 10c) (0-20 μM, 72 h) shows cytotoxicity and anti-proliferative activity against MCF-7, MDA-MB-231, A549, NCI-H1581, H2228, Hep3B, and RAW264.7 cells^[1].
ATX inhibitor 13 (0-1 μM, 0-72 h) inhibits migration of RAW264.7 cells in a dose-dependent manner, significantly down-regulates both the colony count and colony single area with the concentration elevation^[1].
ATX inhibitor 13 (0-1 μM, 72 h) dose dependently suppresses colony formation of RAW264.7 cells^[1].
ATX inhibitor 13 (0-1 μM, 48 h) induces weak apoptosis in a dose-dependent manner in RAW264.7 cells^[1].
ATX inhibitor 13 (0-1 μM, 48 h) brings G2 phase arrest of RAW264.7 cells^[1].

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

Cell Proliferation Assay

Cell Line:

MCF-7, MDA-MB-231, A549, NCI-H1581, H2228, Hep3B, RAW264.7^[1]
Concentration:

0-20 μM
Incubation Time:

72 h
Result:

Showed cytotoxicity and antiproliferative activity against MCF-7, MDA-MB-231, A549, NCI-H1581, H2228, Hep3B, and RAW264.7 cell lines, with IC₅₀ values of 3.87 ± 0.37, 3.29 ± 0.37, 6.59 ± 0.26, 4.76 ± 0.57, 4.27 ± 0.21, 0.58 ± 0.11, and 0.63 ± 0.26 μM.

Apoptosis Analysis

Cell Line:

RAW264.7 cells^[1]
Concentration:

0 μM, 0.1 μM, 0.25 μM, 0.5 μM and 1 μM
Incubation Time:

48 h
Result:

Induced apoptosis in a dose-dependent manner, with the apoptotic rates of 6.48% (0.1 μM), 7.73% (0.25 μM), 8.60% (0.5 μM) and 9.17% (1 μM).

Cell Cycle Analysis

Cell Line:

RAW264.7 cells^[1]
Concentration:

0 μM, 0.1 μM, 0.25 μM, 0.5 μM and 1 μM
Incubation Time:

24 h
Result:

Led to significant G2 phase arrest in RAW264.7 cells in a dose-dependent manner, the percentage of cells in the G2 phase slightly increased from 10.90% to 90.16% (0-1 μM).

In Vivo

ATX inhibitor 13 (compound 10c) (C57BL/6J mice, 0-1000 mg/kg, Orally, once) has an acceptable safety profile^[1].

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

Animal Model:

C57BL/6J mice (5 groups,4 mice per group)^[1]
Dosage:

5000, 3200, 2500 and 1000 mg/kg
Administration:

Orally, once
Result:

Had an acceptable safety profile, showed no obvious safety concerns.

Chemical Information

CAS No. 2485779-34-6
Molecular Weight 596.55
Formula C₃₁H₃₅Cl₂N₅O₃
SMILES

O=C(OCC1=CC(Cl)=CC(Cl)=C1)NC2=C(CC)N=C3C(C)=CC(C4=CC=C(CN5CCN(CCO)CC5)C=C4)=CN32
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 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)
Handling Instructions (2659 KB)

References

[1]. Lei H, et al. Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors. Eur J Med Chem. 2022;236:114307. [Content Brief]

Calculators

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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.

Keywords

100 mg

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