| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| ln Vitro |
ASX-173 (0.1-1000 nM, 24 hours) inhibited the transcription of multiple endogenous Wnt target genes in HCT-116 cells, including AXIN1, DKK1, CD133/PROM1 and MYC[1]. ASX-173 showed strong cytotoxicity in DMEM medium, but had little or no effect in MDA-MB-231, SW620 and A375 cells cultured in RPMI-1640 medium[1]. ASX-173 (0-500 nM) restored the sensitivity of ASNS-deficient RS4;11 cells to ASNase[1]. ASX-173 (0-1250 nM) enhanced the anticancer activity of ASNase against ASNS-positive cancer cell lines in OPM-2, MOLP-8, AMO-1, Jurkat, H929, MV4;11 and HT1080 cells[1]. ASX-173 (0-1500 nM) enhances the sensitivity of OVCAR-8, 92.1_D3, 92.1_M3 and OCI-AML2 cells when used in combination with ASNaseWT or a glutaminase-deficient ASNase variant (ASNaseQ59L)13 [1]. Under asparagine-deficient conditions, ASX-173 (0-1500 nM) showed anticancer activity against most tested cell lines (e.g., MV4;11, Jurkat, A172) when treated with asparagine-free medium or low dose of asparaginase (0.025 IU/mL) [1]. Under asparagine-deficient conditions, ASX-173 (0-500 nM, 48 h) induces cell cycle arrest in MV4;11 leukemia cells and RS4;11_ASNS cells and activates apoptosis and autophagy [1]. In OCI-AML2 leukemia cells treated with 0.025 IU/mL asparaginase (Spectrila), ASX-173 (80 nM, 24 h) disrupted nucleotide biosynthesis [1].
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| ln Vivo |
ASX-173 (50 mg/kg, orally, once daily for 2 weeks) enhanced the anticancer efficacy of ASNase (5,000 IU/kg, intraperitoneally) in NSG mice transplanted with OCI-AML2 leukemia cells expressing luciferase [1].
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| Cell Assay |
RT-PCR[1]
Cell Types: HCT-116 cells Tested Concentrations: 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM Incubation Duration: 24 hours Experimental Results: The transcription of several endogenous Wnt target genes was inhibited, including AXIN1, DKK1, CD133/PROM1 and MYC. Cell cycle analysis [1] Cell Types: MV4;11 leukemia/RS4;11_ASNS cells Tested Concentrations: 0 nM, 5 nM, 50 nM, 500 nM Incubation Duration: 48 h Experimental Results: No significant changes were observed in cell cycle distribution when treated with asparagine-deficient medium or ASX-173 alone. Under asparagine-deficient conditions, cell cycle dynamics changed significantly, with an increased proportion of cells in sub-G1 phase and a decreased proportion of cells in G2/M and S phases, indicating enhanced cell cycle arrest in G1/G0 phases and leading to apoptosis. Under asparagine-deficient conditions, p27 expression was upregulated and p21 expression was downregulated. Western Blot Analysis [1] Cell Types: MV4;11 Leukemia/RS4;11_ASNS Cells Tested Concentrations: 0 nM, 5 nM, 50 nM, 500 nM Incubation Duration: 48 hours Experimental Results: Under asparagine-deficient conditions, the expression levels of cleaved caspase-3 and cleaved PARP, as well as the phosphorylation levels of AKT, p70S6K, and ERK1/2, were increased. Under asparagine-deficient conditions, the expression of the autophagy marker LC3 was downregulated. |
| Animal Protocol |
Animal/Disease Models:NSG mice transplanted with OCI-AML2 leukemia cells expressing luciferase (0.5 × 10⁶)[1]
Doses: 50 mg/kg + ASNase (5,000 IU/kg, intraperitoneal injection) Route of Administration:Oral, once daily for 2 weeks Experimental Results:Inhibited leukemia progression, while single-drug therapy did not show significant effects. Compared with single-drug therapy, combination therapy delayed leukemia cell growth by 7 days, equivalent to a doubling of leukemia cells by about 3-4 times. Improved overall survival, with all combination therapy groups having a survival period 7-10 days longer than other treatment groups. |
| References |
| Molecular Formula |
C28H30FN3O3
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|---|---|
| Molecular Weight |
475.55
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| CAS # |
2748800-08-8
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| Related CAS # |
(2S,3R,4S)-ASX-173; 2748800-07-7
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| Appearance |
White to off-white solid
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| 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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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~210.28 mM; with sonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.26 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of physiological saline: Dissolve 0.9 g of sodium chloride in double-distilled water and dilute to 100 mL to obtain clear physiological saline. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.26 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD saline (4°C, store for one week): Dissolve 2 g of SBE-β-CD powder in 10 mL of saline until completely dissolved and clear. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.26 mM)(saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1028 mL | 10.5141 mL | 21.0283 mL | |
| 5 mM | 0.4206 mL | 2.1028 mL | 4.2057 mL | |
| 10 mM | 0.2103 mL | 1.0514 mL | 2.1028 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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