STAT5-IN-2是一种具有口服活性的STAT5抑制剂。STAT5-IN-2能够有效阻断STAT5的磷酸化和转录活性。
Cas No.:2111834-61-6
Sample solution is provided at 25 µL, 10mM.
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STAT5-IN-2 is an orally active STAT5 inhibitor. STAT5-IN-2 effectively blocks the phosphorylation and transcriptional activity of STAT5. STAT5-IN-2 is primarily used in scientific research for leukemia and related tumors, and STAT5-IN-2 inhibits the growth of leukemia cells in a concentration-dependent manner[1].
STAT5-IN-2 (1–10μM) pretreatment of Imatinib-resistant K562R cells, Ara-C-resistant MV4-11R cells, and STAT5BN642Hmutant Ba/F3 cells for 24–48 hours, followed by combined treatment with Imatinib (1μM) or Ara-C (1μM), STAT5-IN-2 significantly inhibits STAT5 phosphorylation and transcriptional activity, induces apoptosis, and overcomes chemotherapy resistance[2].
In vivo, STAT5-IN-2 (10mg/kg) administered intraperitoneally every two days to 6-week-old male C57BL/6 mice for 7 days, STAT5-IN-2 did not produce a significant effect on the number of neutrophils and monocytes/macrophages in the peripheral blood of the mice[3].
References:
[1] Juen L, Brachet-Botineau M, Parmenon C, et al. New Inhibitor Targeting Signal Transducer and Activator of Transcription 5 (STAT5) Signaling in Myeloid Leukemias. J Med Chem. 2017 Jul 27;60(14):6119-6136.
[2] Brachet-Botineau M, Deynoux M, Vallet N, et al. A Novel Inhibitor of STAT5 Signaling Overcomes Chemotherapy Resistance in Myeloid Leukemia Cells. Cancers (Basel). 2019 Dec 17;11(12):2043.
[3] Zhang M, Meng Y, Ying Y, et al. Selective activation of STAT3 and STAT5 dictates the fate of myeloid progenitor cells. Cell Death Discov. 2023 Jul 28;9(1):274.
STAT5-IN-2是一种具有口服活性的STAT5抑制剂。STAT5-IN-2能够有效阻断STAT5的磷酸化和转录活性。STAT5-IN-2主要用于白血病及相关肿瘤的科学研究，STAT5-IN-2能以浓度依赖的方式抑制白血病细胞的生长[1]。
STAT5-IN-2（1–10μM）预处理Imatinib耐药K562R细胞、Ara-C耐药MV4-11R细胞及STAT5BN642H突变Ba/F3细胞24–48h，随后联合Imatinib（1μM）或Ara-C（1μM）处理，STAT5-IN-2显著抑制STAT5磷酸化与转录活性，同时诱导细胞凋亡并克服化疗耐药性[2]。
在体内，STAT5-IN-2（10mg/kg）每两日一次腹腔注射，用于处理6周龄C57BL/6雄性小鼠，持续7天。STAT5-IN-2对小鼠外周血中性粒细胞和单核/巨噬细胞数量未产生显著影响[3]。
| Cell experiment [1]: | |
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Cell lines |
K562 cells (human chronic myeloid leukemia cell line), MV4-11 cells (human acute myeloid leukemia cell line) |
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Preparation Method |
K562 and MV4-11 cells, including their respective Imatinib (IM)-resistant (K562R) and Cytarabine (Ara-C)-resistant (MV4-11R) sublines, were maintained in RPMI 1640 medium supplemented with 10% fetal bovine serum (FBS). Cells were treated with STAT5-IN-2 (1-10μM) at specified concentrations, either alone or in combination with IM (1µM) or Ara-C (1µM). |
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Reaction Conditions |
1-10μM; 24h or 48h |
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Applications |
STAT5-IN-2 selectively inhibited STAT5 phosphorylation and transcriptional activity. STAT5-IN-2 strongly inhibited the growth and survival of chemotherapy-resistant CML and AML cells when combined with IM or Ara-C, respectively. STAT5-IN-2 induced apoptosis and cell cycle arrest (G0 phase) in resistant cells. Furthermore, STAT5-IN-2 specifically reduced STAT5B protein expression in resistant cells and suppressed the expression of the oncogenic STAT5BN642H mutant in transformed hematopoietic cells. |
| Animal experiment [2]: | |
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Animal models |
C57BL/6 mice |
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Preparation Method |
Mice were intraperitoneally administered STAT5-IN-2 at 10mg/kg every 2 days for 7 days. Peripheral blood cells were isolated and analyzed by flow cytometry to quantify CD11b+ Ly6G+ neutrophils and CD11b+ F4/80+ monocytes/macrophages. |
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Dosage form |
10mg/kg; i.p.; Administered every 2 days for 7 days. |
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Applications |
STAT5-IN-2 treatment did not produce a significant effect on the number of neutrophils and monocytes/macrophages in the peripheral blood of mice compared to the control group. The lack of observable effect may be attributed to the complexity of the in-vivo microenvironment and/or the low basal phosphorylation level of STAT5 in peripheral blood cells, making its inhibition difficult to detect at the cellular population level. |
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References: |
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| Cas No. | 2111834-61-6 | SDF | Download SDF |
| 分子式 | C26H27N3O | 分子量 | 397.51 |
| 溶解度 | DMSO : 100 mg/mL (251.57 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5157 mL | 12.5783 mL | 25.1566 mL |
| 5 mM | 503.1 μL | 2.5157 mL | 5.0313 mL |
| 10 mM | 251.6 μL | 1.2578 mL | 2.5157 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
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1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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- Purity: >99.00% Appearance: A solid
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