2. Apoptosis
  3. Apoptosis
  4. 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.

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ATX inhibitor 13 Chemical Structure

ATX inhibitor 13 Chemical Structure

CAS No. : 2485779-34-6

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ATX inhibitor 13 Related Antibodies

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Description

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[1].

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.

ATX inhibitor 13 Related Antibodies

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.
Molecular Weight

596.55

Formula

C31H35Cl2N5O3
CAS No.
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
References
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ATX inhibitor 13 Related Classifications

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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:

ATX inhibitor 132485779-34-6ATX inhibitor13ATX inhibitor-13ApoptosisAntitumorallostericLow toxicityOrally activeLeukemia cellsRAW264.7 cellsInhibitorinhibitorinhibit

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