上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
JNJ-38158471
JNJ-38158471 是一种耐受良好，有口服活性的高选择性 VEGFR-2 抑制剂，IC50 值为 40 nM。JNJ-38158471 还抑制 Ret 和 Kit ，IC50 值分别为 180 和 500 nM。
JNJ-38158471 Chemical Structure
CAS No. : 951151-97-6
| 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 |
JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively[1].
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| IC50 & Target[1] |
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VEGFR-2
40 nM (IC50)
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RET
180 nM (IC50)
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c-Kit
500 nM (IC50)
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体外研究
(In Vitro) |
JNJ-38158471 (1-500 nM; 1 hour) inhibits VEGF-stimulated VEGFR-2 autophosphorylation in HUVECs[1].
JNJ-38158471 (50-1000 nM; 12-16 hours) significantly inhibits VEGF-dependent HUVEC migration. Cellular toxicity is not observed following JNJ-38158471 treatment of HUVECs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis[1]
| Cell Line: |
Human umbilical vein endothelial cells (HUVECs) |
| Concentration: |
1, 10, 100, 500 nM |
| Incubation Time: |
1 hour |
| Result: |
Reduced phospoho-VEGFR2 levels at 95, 88, 77 and 73% with the concentration of 500, 100, 10 and 1 nM, respectively. |
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体内研究
(In Vivo) |
JNJ-38158471 (10 or 100 mg/kg; p.o.; once-daily) inhibits VEGF-induced corneal neovascularization[1].
JNJ-38158471 (10-200 mg/kg; p.o.) inhibits the growth of human tumor xenografts in a dose-dependent manner in both A431 and HCT116 models. JNJ-38158471 treatment is well tolerated, following continuous administration for 24 days, body weights were comparable with control animals[1].
JNJ-38158471 (100 mg/kg; p.o.; once-daily) treatment shows statistically significant activity compare with vehicle treat animals. The body weights of both JNJ-38158471-treated and vehicle-treated groups were comparable at study end[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
Female C57BL/6J mice are implanted with rhVEGF165[1] |
| Dosage: |
10 or 100 mg/kg |
| Administration: |
Daily oral administration for 6 days |
| Result: |
Caused a marked and apparently dose-dependent inhibition of VEGF-dependent blood vessel formation (100 mg/kg, resulted in 83% inhibition; 10 mg/kg, resulted in 15% inhibition). |
| Animal Model: |
Female athymic nude mice; 5-6 weeks; implanted subcutaneously human colorectal carcinoma cells (HCT116) or human epidermoid carcinoma cells (A431)[1] |
| Dosage: |
10, 50, 100, 200 mg/kg |
| Administration: |
Oral administration for 35 days |
| Result: |
Achieved optimum efficacy with the dose from 100 to 200 mg/kg daily. |
| Animal Model: |
Female athymic nude mice; 5-6 weeks; implanted subcutaneously human skin melanoma cells (A375)[1] |
| Dosage: |
100 mg/kg |
| Administration: |
Once-daily oral administration for 28 days |
| Result: |
Inhibited 90% growth of tumor with daily doses of 100 mg/kg. |
| Animal Model: |
Female C57BL/6J-Apc Min mice; 5 weeks of age[1] |
| Dosage: |
100 mg/kg |
| Administration: |
Once-daily oral administration for two weeks |
| Result: |
Inhibited polyp formation in the transgenic APC min-mouse model. |
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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]. Kenneth RL, et, al. A Highly Selective, Orally Bioavailable, Vascular Endothelial Growth Factor receptor-2 Tyrosine Kinase Inhibitor Has Potent Activity in Vitro and in Vivo. Angiogenesis. 2009; 12(3): 287-96.
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