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GSK143 dihydrochloride
GSK143 dihydrochloride 是一种具有口服活性，高选择性的脾酪氨酸激酶 (SYK) 抑制剂，pIC50 为 7.5。GSK143 dihydrochloride 抑制 Erk 磷酸化 (pErk: pIC50=7.1)。GSK143 dihydrochloride 可以减轻炎症，并防止小鼠肠道肌层中免疫细胞的募集。
GSK143 dihydrochloride Chemical Structure
CAS No. : 2341796-81-2
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: pIC50=7.1)[1]. GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice[2][3].
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IC50 & Target |
pIC50: 7.5 (SYK) and 7.1 (pErk)[1]
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体外研究
(In Vitro) |
GSK143 dihydrochloride (compound 20) inhibits ZAP-70 (pIC50=4.7), LCK (pIC50=5.3), LYN (pIC50=5.4), JAK1/2/3 (pIC50=5.8/5.8/5.7), Aurora B (pIC50=4.8), hWB (pIC50=6.6), hERG (pIC50=4.7)[1].
GSK143 dihydrochloride (10-10000 nM; every 24 hours for 3 days) has an IC50 of 323 nM in CLL cells. GSK 143 dihydrochloride (1 μM; 30 mins) abrogates early signalling events including SYK phosphorylation and calcium flux[2].
GSK143 dihydrochloride (0.1-10 μM; for 30 min) reduces cytokine expression in bone marrow derived macrophages in a concentration-dependent manner[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[2]
| Cell Line: |
Chronic lymphocytic leukaemia (CLL) cells |
| Concentration: |
10, 100, 1000, 10000 nM |
| Incubation Time: |
Every 24 hours for 3 days |
| Result: |
Had an IC50 of 323 nM. |
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体内研究
(In Vivo) |
GSK143 (0.1-10 mg/kg; orally; 1.5 hours) reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis of 1 mg/kg[3].
GSK143 (3, 10, 30, 100 mg/kg; oral; 1 hour before ovalbumin challenge) reduces the cutaneous reverse passive Arthus reaction in a dose dependent manner by approximately 50% and 70% at 10 mg/kg and 30 mg/kg, respectively[2].
GSK143 (iv of 1 mg/kg; po of 3 mg/kg) has a T1/2 of 4.2 hours, low clearance (16 mL/min/kg), moderate bioavailability of 30% and a Vss of 4.1 L/kg in rats[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
Wild type C57NL/BL6 mice, 10-12 weeks old[3] |
| Dosage: |
0.1, 1, 3, 10 mg/kg |
| Administration: |
Orally; 1.5 hours before intestinal manipulation (IM) |
| Result: |
Reduced inflammation and prevented recruitment of immune cells in the intestinal muscularis. |
| Animal Model: |
Male CD rats (175-200 g)[1] |
| Dosage: |
1 mg/kg of iv; 3 mg/kg of po (Pharmacokinetic Analysis) |
| Administration: |
IV or PO |
| Result: |
Had a T1/2 of 4.2 hours, low clearance (16 mL/min/kg), moderate bioavailability of 30% and a Vss of 4.1 L/kg. |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. John Liddle, et al. Discovery of GSK143, a Highly Potent, Selective and Orally Efficacious Spleen Tyrosine Kinase Inhibitor. Bioorg Med Chem Lett. 2011 Oct 15;21(20):6188-94.
[2]. Abraham M Varghese, et al. Highly Selective SYK Inhibitor, GSK143, Abrogates Survival Signals in Chronic Lymphocytic Leukaemia. Br J Haematol. 2018 Sep;182(6):927-930.
[3]. Sjoerd H W van Bree, et al. Inhibition of Spleen Tyrosine Kinase as Treatment of Postoperative Ileus. Gut. 2013 Nov;62(11):1581-90.
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