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 是一种具有口服活性的天冬酰胺合成酶 (ASNS) 抑制剂 (IC50 = 0.113 μM, Ki = 0.4 nM)。ASX-173 增强 L-Asparaginase (ASNase) (HY-P1923) 的抗癌活性。ASX-173 与 ASNase 联用可破坏核苷酸合成，并诱导白血病细胞周期停滞、凋亡 (apoptosis) 和自噬 (autophagy)。ASX-173 与 ASNase 联用可延缓 OCI-AML2 异种移植瘤的生长。ASX-173 可用于急性淋巴细胞白血病、急性髓性白血病、结直肠癌等癌症的研究。

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ASX-173

ASX-173 Chemical Structure

CAS No. : 2748800-08-8

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ASX-173 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

ASX-173 (0.1-1000 nM，24 小时) 可抑制 HCT-116 细胞中多个内源性 Wnt 靶基因的转录，包括 AXIN1、DKK1、CD133/PROM1 和 MYC[1]。
ASX-173 对于 MDA-MB-231、SW620 和 A375 细胞，在 DMEM 培养基中培养表现出强效细胞毒性，但在 RPMI-1640 培养基中，其毒性极小甚至无毒性[1]。
ASX-173 (0-500 nM) 可恢复 ASNS 缺陷型 RS4;11 细胞对 ASNase (HY-P1923) 的敏感性[1]。
ASX-173 (0-1250 nM) 可增强 ASNase 在 ASNS 阳性癌细胞系 OPM-2、MOLP-8、AMO-1、Jurkat、H929、MV4;11、HT1080 细胞中的抗癌活性[1]。
ASX-173 (0-1500 nM) 在 OVCAR-8、92.1_D3、92.1_M3 和 OCI-AML2 细胞中可提高与 ASNaseWT 或谷氨酰胺酶缺陷型 ASNase 变体 (ASNaseQ59L)13 的结合敏感性[1]。
ASX-173 (0-1500 nM) 在缺乏 Asparagine (HY-N0667) 的条件下，使用不含 Asparagine 的中剂量或低剂量 ASNase (0.025 IU/mL)， 对大多数受试细胞系 (例如：MV4;11、Jurkat、A172) 均显示出抗癌活性[1]。
ASX-173 (0-500 nM, 48 小时) 在缺乏 Asparagine 的条件下，可诱导 MV4;11 白血病细胞和 RS4;11_ASNS 细胞的细胞周期停滞并激活凋亡和自噬[1]。
ASX-173 (80 nM，24 小时) 在用 0.025 IU/mL ASNase (Spectrila) 处理的 OCI-AML2 白血病细胞中，可破坏核苷酸生物合成[1]。

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

ASX-173 相关抗体:

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.
体内研究
(In Vivo)

ASX-173 (50 mg/kg，口服，每日一次，2 周) 可增强 ASNase (5,000 IU/kg，腹腔注射) 在异种移植了表达荧光素酶的 OCI-AML2 白血病细胞的 NSG 小鼠中的抗癌功效[1]。

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.
分子量

475.55

Formula

C28H30FN3O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

ASX-173 相关分类

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  • 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:

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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