2. Apoptosis Cell Cycle/DNA Damage Epigenetics PI3K/Akt/mTOR Autophagy
  3. Apoptosis Caspase CDK PARP Akt Autophagy Atg8/LC3
  4. ASX-173

ASX-173 is an orally active inhibitor of asparagine synthetase (ASNS) (IC50 = 0.113 μM, Ki = 0.4 nM). ASX-173 enhances the anticancer activity of L-asparaginase (ASNase) (HY-P1923). ASX-173 disrupts nucleotide synthesis and induces leukemia cell cycle arrest, apoptosis and autophagy in leukemia cells in combination with ASNase. ASX-173 slows the growth of OCI-AML2 xenografts in combination with ASNase. ASX-173 is indicated for the study of acute lymphoblastic leukemia, acute myeloid leukemia, colorectal cancer, and other cancers.

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ASX-173

ASX-173 Chemical Structure

CAS No. : 2748800-08-8

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ASX-173 Related Antibodies

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Description

ASX-173 is an orally active inhibitor of asparagine synthetase (ASNS) (IC50 = 0.113 μM, Ki = 0.4 nM). ASX-173 enhances the anticancer activity of L-asparaginase (ASNase) (HY-P1923). ASX-173 disrupts nucleotide synthesis and induces leukemia cell cycle arrest, apoptosis and autophagy in leukemia cells in combination with ASNase. ASX-173 slows the growth of OCI-AML2 xenografts in combination with ASNase. ASX-173 is indicated for the study of acute lymphoblastic leukemia, acute myeloid leukemia, colorectal cancer, and other cancers[1].

IC50 & Target[1]

Caspase 3

 

In Vitro

ASX-173 (0.1-1000 nM,24 h) suppresses transcription of several endogenous Wnt target genes, including AXIN1, DKK1, CD133/PROM1, and MYC in HCT-116 cells[1].
ASX-173 exhibits potent cytotoxicity in DMEM medium but minimal to no effect when cells were cultured in RPMI-1640 in MDA-MB-231, SW620, A375 cells[1].
ASX-173 (0-500 nM) restores sensitivity to ASNase (HY-P1923) in ASNS-deficient RS4;11 cells[1].
ASX-173 (0-1250 nM) enhances the ASNS-positive cancer cell lines anticancer activity of ASNase in OPM-2, MOLP-8, AMO-1, Jurkat, H929, MV4;11, HT1080 cells[1].
ASX-173 (0-1500 nM) increases sensitivity combination with ASNaseWT or a glutaminase-deficient ASNase variant (ASNaseQ59L)13 in OVCAR-8, 92.1_D3, 92.1_M3 and OCI-AML2 cells[1].
ASX-173 (0-1500 nM) shows anticancer activity of majority of tested lines (such as: MV4;11, Jurkat, A172) under Asparagine (HY-N0667)-deprived conditions, using either asparagine-free medium or low-dose ASNase (0.025 IU/mL)[1].
ASX-173 (0-500 nM, 48 h) induces cell cycle arrest and activates apoptosis and autophagy under Asparagine-depleted conditions in MV4;11 leukemia and RS4;11_ASNS cells[1].
ASX-173 (80 nM, 24 h) disrupts nucleotide biosynthesis in OCI-AML2 leukemia cells treated with 0.025 IU/mL ASNase (Spectrila)[1].

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

ASX-173 Related Antibodies

RT-PCR[1]

Cell Line: HCT-116 cells
Concentration: 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time: 24 h
Result: Suppressed transcription of several endogenous Wnt target genes, including AXIN1, DKK1, CD133/PROM1, and MYC.

Cell Cycle Analysis[1]

Cell Line: MV4;11 leukemia/RS4;11_ASNS cells
Concentration: 0 nM, 5 nM, 50 nM, 500 nM
Incubation Time: 48 h
Result: Did not significantly alter cell cycle distribution when asparagine-deficient media or ASX-173 treatment alone.
Led to pronounced changes in cell cycle dynamics, increased the sub-G1 population accompanied and decreased G2/M and S phase populations, indicating enhanced cell cycle arrest in G1/G0 and apoptotic cell death under Asparagine-deprived conditions.
Up-regulated p27, down-regulated p21 under Asparagine-deprived conditions.

Western Blot Analysis[1]

Cell Line: MV4;11 leukemia/RS4;11_ASNS cells
Concentration: 0 nM, 5 nM, 50 nM, 500 nM
Incubation Time: 48 h
Result: Increase the expression levels of cleaved caspase-3 , cleaved PARP and phosphorylation of AKT, p70S6K, and ERK1/2 under Asparagine-deprived conditions.
Down-regulated the autophagic marker LC3 under Asparagine-deprived conditions.
In Vivo

ASX-173 (50 mg/kg, p.o., once a day, 2 weeks) potentiates anticancer efficacy of ASNase (5,000 IU/kg, i.p.) anticancer efficacy in NSG mice xenografted with luciferase-expressing OCI-AML2 leukemia cells[1].

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

Animal Model: NSG mice xenografted with luciferase-expressing OCI-AML2 leukemia cells (0.5 × 106)[1]
Dosage: 50 mg/kg + ASNase (5,000 IU/kg, i.p.)
Administration: p.o., once a day, 2 weeks
Result: Suppressed leukemia progression, whereas monotherapy with either agent showed no significant effect.
Achieved a 7-day growth delay over the monotherapies, representing approximately 3-4 leukemia doubling times.
Improved overall survival, with all combination-treated mice living 7-10 days longer than those in other treatment groups.
Molecular Weight

475.55

Formula

C28H30FN3O3
CAS No.
SMILES

CC[C@@H](C(N1C[C@@H](C2=CC=C(C=C2)F)[C@H](O)[C@@H]1C(NC(C3=CC=CC=C3)C4=CC=CC=C4)=O)=O)N
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ASX-173 Related Classifications

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    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:

ASX-1732748800-08-8ASX173ASX 173ApoptosisCaspaseCDKPARPAktAutophagyAtg8/LC3Cyclin dependent kinasepoly ADP ribose polymerase PKBProtein kinase BAutophagy-related 8| InhibitorHCT-116 cellsRS4;11-ASNS cellsOCI-AML2 leukemia cellsleukemiaNSG miceInhibitorinhibitorinhibit

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