1. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt
  2. JAK STAT
  3. HAT-SIL-TG-1&AT

HAT-SIL-TG-1&AT 是一种 Janus 酪氨酸激酶 (JAK) 抑制剂,具有抗肿瘤作用。HAT-SIL-TG-1&AT 是缺氧激活的前药,可抑制肿瘤组织中的 JAK-STAT 信号传导。HAT-SIL-TG-1&AT 在低氧条件下抑制 HEL 细胞增殖并下调磷酸化的 STAT3/5

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HAT-SIL-TG-1&AT Chemical Structure

HAT-SIL-TG-1&AT Chemical Structure

CAS No. : 2973282-50-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HAT-SIL-TG-1&AT is a Janus tyrosine kinase (JAK) inhibitor with antitumor effects. HAT-SIL-TG-1&AT is the hypoxia-activated prodrug, witch inhibits JAK-STAT signaling in tumor tissue. And HAT-SIL-TG-1&AT inhibits HEL cells proliferation and downregulated phosphorylated STAT3/5 under hypoxic conditions[1].

IC50 & Target[1]

STAT3

 

STAT5

 

体外研究
(In Vitro)

HAT-SIL-TG-1&AT 在缺氧条件下可在细胞裂解物中以 TG-1 和 AT 的形式释放[1]
HAT-SIL-TG-1&AT (1-5 μM; 24 h) 抑制 HEL 细胞中 STAT3/5 的磷酸化,在 3 μM 时显着抑制[1]

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

Western Blot Analysis[1]

Cell Line: HEL cells
Concentration: 3 μM, 5 μM
Incubation Time: 24 h
Result: Competely inhibited STAT3 phorphoslation at 3 μM and significantly inhibited STAT5 phorphoslation at 5 μM.
体内研究
(In Vivo)

HAT-SIL-TG-1&AT (80 mg/kg;腹腔注射;每天一次,持续 14 天) 在 HEL 肿瘤异种移植雄性 Balb/c 裸鼠中表现出显着的肿瘤生长抑制。HAT-SIL-TG-1&AT 还诱导小鼠细胞凋亡[1]

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

Animal Model: HEL tumors xenograft male Balb/c-nude mice[1]
Dosage: 40 mg/kg, 80 mg/kg
Administration: Intraperitoneal injection; once daily for 14 days
Result: Resulted regression on tumor growth with TGI values of 88.9% and 91.2%, respectively.
分子量

1236.36

Formula

C60H69N17O11S

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
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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.

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产品名称:
HAT-SIL-TG-1&AT
目录号:
HY-149257
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