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（ 母液浓度为 40 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们客服联系。| 中文名称: | BMS-599626 hydrochloride 一键复制产品信息 | ||||
|---|---|---|---|---|---|
| 英文名称: | BMS-599626 hydrochloride | ||||
| 别名: | BMS-599626 hydrochloride (S)-morpholin-3-ylmethyl (4-((1-(3-fluorobenzyl)-1H-indazol-5-yl)amino)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)carbamate hydrochloride | ||||
| CAS No: | 873837-23-1 | 分子式: | C27H28ClFN8O3 | 分子量: | 567.01 |
| CAS No: | 873837-23-1 | ||||
| 分子式: | C27H28ClFN8O3 | ||||
| 分子量: | 567.01 | ||||
包装规格：
5mg 10mg 25mg 50mg 100mg in glass bottle
产品简介：
一种选择性的口服生物利用度HER1和HER2抑制剂，其IC50分别为20和30nM。BMS-599626 hydrochloride对HER4的IC50值为190nM，对VEGFR2、c-Kit、Lck、MEK的抑制强度降低了100倍。BMS-599626 hydrochloride抑制肿瘤细胞增殖，并有可能增加肿瘤对放疗的反应。
溶解性：
溶于DMSO（100mg/ml超声）
储备液保存：
-80°C, 6 months
-20°C, 1 month
(sealed storage, away from moisture)
-20°C, 1 month
(sealed storage, away from moisture)
体内实验：
1、请依序添加每种溶剂： 10% DMSO→40% PEG300→5% Tween-80→45% Saline
Solubility: ≥ 2.5 mg/mL (4.41 mM); 澄清溶液
此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。
2、请依序添加每种溶剂： 10% DMSO→90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.41 mM); 澄清溶液
此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。
3、请依序添加每种溶剂： 10% DMSO→ 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.41 mM); 澄清溶液
此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。
Solubility: ≥ 2.5 mg/mL (4.41 mM); 澄清溶液
此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。
2、请依序添加每种溶剂： 10% DMSO→90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.41 mM); 澄清溶液
此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。
3、请依序添加每种溶剂： 10% DMSO→ 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.41 mM); 澄清溶液
此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。
体外研究：
BMS-599626 Hydrochloride inhibits the proliferation of tumor cells that are dependent on HER1/HER2 signaling.BMS-599626 Hydrochloride (0.03-8 μM; 1 huors) results in the inhibition of receptor autophosphorylation, as well as MAPK phosphorylation, with IC50s of 0.3 and 0.22 μM, respectively, in Sal2 cells which express a CD8HER2 fusion protein.
BMS-599626 Hydrochloride abrogates HER1 and HER2 signaling and inhibited the proliferation of tumor cell lines that are dependent on these receptors, with IC50s in the range of 0.24 to 1 μM.In GEO cells, HER1 phosphorylation is stimulated by treatment with EGF and is inhibited by BMS-599626 Hydrochloride (IC50=0. 75 μM).There is also nearly complete inhibition of EGF-dependent MAPK (0. 8 μM) but only partial inhibition of AKT signaling.The latter likely reflects the activation of AKT by multiple upstream signals.Treatment of N87 cells with BMS-599626 Hydrochloride leads to the inhibition of HER2 (0. 38 μM), which is expressed to a high level because of gene amplification, as well as MAPK and AKT phosphorylation (0.35 μM for both).
At the molecular level, in HN-5 cells the agent (BMS-599626 Hydrochloride) inhibits the expression of pEGFR, pHER2, cyclins D and E, pRb, pAkt, pMAPK, pCDK1 and 2, CDK 6, and Ku70 proteins. BMS-599626 Hydrochloride also induced accumulation of cells in the G1 cell cycle phase, inhibited cell growth, enhanced radiosensitivity, and prolonged the presence of γ-H AX foci up to 24 h after radiation.
BMS-599626 Hydrochloride abrogates HER1 and HER2 signaling and inhibited the proliferation of tumor cell lines that are dependent on these receptors, with IC50s in the range of 0.24 to 1 μM.In GEO cells, HER1 phosphorylation is stimulated by treatment with EGF and is inhibited by BMS-599626 Hydrochloride (IC50=0. 75 μM).There is also nearly complete inhibition of EGF-dependent MAPK (0. 8 μM) but only partial inhibition of AKT signaling.The latter likely reflects the activation of AKT by multiple upstream signals.Treatment of N87 cells with BMS-599626 Hydrochloride leads to the inhibition of HER2 (0. 38 μM), which is expressed to a high level because of gene amplification, as well as MAPK and AKT phosphorylation (0.35 μM for both).
At the molecular level, in HN-5 cells the agent (BMS-599626 Hydrochloride) inhibits the expression of pEGFR, pHER2, cyclins D and E, pRb, pAkt, pMAPK, pCDK1 and 2, CDK 6, and Ku70 proteins. BMS-599626 Hydrochloride also induced accumulation of cells in the G1 cell cycle phase, inhibited cell growth, enhanced radiosensitivity, and prolonged the presence of γ-H AX foci up to 24 h after radiation.
体内研究：
BMS-599626 Hydrochloride (60-240 mg/kg; p.o.; daily for 14 days) results in a dose-dependent inhibition of Sal2 tumor growth.
BMS-599626 Hydrochloride treatment results in the inhibition of GEO xenograft tumor growth when given once daily for 14 days. In addition to efficacy in the Sal2, GEO, and KPL4 models, BMS-599626 has similar antitumor activity in other HER2 amplified xenograft models including the BT474 breast and N87 gastric tumors, as well as other HER1-overexpressing non-small-cell lung tumors (A549 and L2987).
BMS-599626 Hydrochloride given before and during irradiation improved the radioresponse of HN5 tumors in vivo.
BMS-599626 Hydrochloride treatment results in the inhibition of GEO xenograft tumor growth when given once daily for 14 days. In addition to efficacy in the Sal2, GEO, and KPL4 models, BMS-599626 has similar antitumor activity in other HER2 amplified xenograft models including the BT474 breast and N87 gastric tumors, as well as other HER1-overexpressing non-small-cell lung tumors (A549 and L2987).
BMS-599626 Hydrochloride given before and during irradiation improved the radioresponse of HN5 tumors in vivo.
保存条件：
-20℃
注意事项：
1、为了您的安全和健康，请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
UN码：
HazardClass：
危害声明：
安全说明：
搜索质检报告(COA)
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
(2).jpg)
体内配方的制备方法: 取 50μLDMSO 母液，添加 300 μLPEG300 混匀澄清，再加 50μLTween80, 混匀澄清，再加 600μLSaline/PBS/ddH2O 混匀澄清
方案所需的各种助溶剂如： DMSO ， PEG300 / PEG400 ， Tween 80 ， SBE-β-CD ， 玉米油 等， 均可点击跳转或在网站搜索购买。
母液，添加 300 μLPEG300 混匀澄清，再加 50μLTween80, 混匀澄清，再加 600μLSaline/PBS/ddH2O 混匀澄清方案所需的各种助溶剂如： DMSO ， PEG300 / PEG400 ， Tween 80 ， SBE-β-CD ， 玉米油 等， 均可点击跳转或在网站搜索购买。
以上为“动物实验计算换算器”的使用方法举例，并不是具体某个试剂的配制，请根据您的实验动物和给药方式选择适当的溶解方案。
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL Saline/PBS/ddH2O，混匀澄清。
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。
剂量转换
对于不同动物的给药剂量换算，您也可以参考 更多
