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。
BMS-754807 纯度: 99.76%
BMS-754807 是有效、可逆的 IGF-1R/IR 抑制剂,其 IC50 值分别为 1.8 和 1.7 nM,Ki 值均小于 2 nM。BMS-754807 同时也抑制 Met,RON,TrkA,TrkB,AurA 和 AurB 的活性,IC50 值分别为 6,44,7,4,9 和 25 nM。
BMS-754807 Chemical Structure
CAS No. : 1001350-96-4
规格 | 价格 | 是否有货 | 数量 |
---|---|---|---|
10 mM * 1 mL in DMSO | ¥1320 | In-stock | |
5 mg | ¥1200 | In-stock | |
10 mg | ¥1900 | In-stock | |
25 mg | ¥3800 | In-stock | |
50 mg | ¥6200 | In-stock | |
100 mg | ¥9800 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
* Please select Quantity before adding items.
BMS-754807 相关产品
•相关化合物库:
- Drug Repurposing Compound Library Plus
- Clinical Compound Library Plus
- Bioactive Compound Library Plus
- Kinase Inhibitor Library
- Protein Tyrosine Kinase Compound Library
- Anti-Cancer Compound Library
- Clinical Compound Library
- Anti-Aging Compound Library
- Drug Repurposing Compound Library
- Differentiation Inducing Compound Library
- Endocrinology Compound Library
- Anti-Lung Cancer Compound Library
- Anti-Pancreatic Cancer Compound Library
- Angiogenesis Related Compound Library
生物活性 |
BMS-754807 is a potent and reversible IGF-1R/IR inhibitor (IC50=1.8 and 1.7 nM, respectively; Ki=<2 nm for both). bms-754807 also shows potent activities against met, ron, trka, trkb, aura, and aurb with IC50 values of 6, 44, 7, 4, 9, and 25 nM, respectively[1]. |
IC50 & Target |
IC50: 1.7 nM (IR), 1.8 nM (IGF-1R), 4 nM (TrkB), 6 nM (Met), 7 nM (TrkA), 9 nM (AurA), 25 nM (AurB), 44 nM (RON)[1] |
||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
体外研究 (In Vitro) |
BMS-754807 effectively inhibits the growth of a broad range of human tumor cell lines with IC50 values of ranging from 5 to 365 nM. BMS-754807 also inhibits the proliferation of human rhabdomyosarcoma tumor cells Rh41 and human colon carcinoma Geo with IC50s of 7 and 5 nM, respectively. BMS-754807 shows inhibitory activity in the proliferation of Rh41 cells with IC50 of 5 nM[1]. BMS-754807 inhibits the phosphorylation of IGF-1R (IC50=13 nM) and the downstream targets Akt (IC50=22 nM) and MAPK (IC50=13 nM) in the IGF-Sal cell line with IC50 consistent with the antiproliferative IC50 (7 nM) in this cell line[2]. BMS-754807 shows a median EC50 value of 0.62 μM against the PPTP cell lines. The median EC50 for the four Ewing sarcoma cell lines is less than that for the remaining PPTP cell lines (0.19 μM vs. 0.78 μM, P=0.0470)[3]. BMS-754807 (0.25 and 0.5 μM) reduces the activated IGF-IR/IR (pIGF-IR/IR), causes a concurrent decrease in phosphorylated AKT in both lung cancer cell lines. BMS-754807 (0.5 μM) also reduces wound closure of lung cancer cells and reduces the ERK phosphorylation. BMS-754807 reduces cell viability in both A549 and NCI-H358 cells, with IC50 of 1.08 μM and 76 μM, respectively[4]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||||||
体内研究 (In Vivo) |
BMS-754807 (3.125 and 12.5 mg/kg, p.o.) inhibits tumor growth in IGF-1R-Sal tumor-bearing nude mice. BMS-754807 inhibits tumor growth in a selected group of epithelial (IGF-1R-Sal, GEO, and Colo205), hematopoietic (JJN3), and mesenchymal (RD1 and Rh41) xenograft tumor models with TGI ranging from 53% to 115%. BMS-754807 is effective at a dose level of 3.125 mg/kg twice daily and as low as 6.25 mg/kg once daily, in the highly sensitive Rh41 rhabdomyosarcoma. BMS-754807 (25 mg/kg) also shows synergy when combined with targeted agents in human tumor cell lines and human xenograft models[1]. Furthmore, BMS-754807 is active at doses from 3 mg/kg upward in the IGF-Sal tumor model[2]. BMS-754807 (25 mg/kg, p.o.) induces significant differences in EFS distribution compared to controls in 18 of 32 evaluable solid tumor xenografts (56%) tested, but in none of the ALL xenografts studied[3]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||||||
Clinical Trial |
|
||||||||||||||||
分子量 |
461.49 |
||||||||||||||||
Formula |
C23H24FN9O |
||||||||||||||||
CAS 号 |
1001350-96-4 |
||||||||||||||||
运输条件 |
Room temperature in continental US; may vary elsewhere. |
||||||||||||||||
储存方式 |
|
||||||||||||||||
溶解性数据 |
In Vitro:
DMSO : ≥ 100 mg/mL (216.69 mM) * “≥” means soluble, but saturation unknown. 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
|
||||||||||||||||
参考文献 |
|
Cell Assay [1] |
Cells are grown at their optimal density in RPMI+GlutaMax. Cell proliferation is evaluated by incorporation of 3H-thymidine into DNA after exposure of cells to BMS-754807 for 72 h. Results are expressed as an IC50, which is the drug concentration required to inhibit cell proliferation by 50% compared with untreated control cells. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
---|---|
Animal Administration [1] |
The required numbers of animals needed to detect a meaningful response are pooled at the start of the experiment and each is given a subcutaneous implant of a tumor fragment (appr 20 mg) with a 13-gauge trocar. Tumors are allowed to grow to the predetermined size window (75-200 mg; tumors outside the range are excluded), and animals are evenly distributed to various treatment and control groups. There are typically eight mice per treatment and control groups, with the exception of experiments conducted in the Sal-IGF (same as IGF-1R-Sal) tumor model, in which there are typically five mice per treatment and control group. Treatment of each animal is based on individual body weight. Treated animals are checked daily for treatment-related toxicity/mortality. Each group of animals is weighed before the initiation of treatment (Wt1) and then again following the last treatment dose (Wt2). The difference in body weight (Wt2 − Wt1) provides a measure of treatment-related toxicity. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
|
所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务