规格 | 价格 | 库存 | 数量 |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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体外研究 (In Vitro) |
在人 LN-308 和鼠 SMA-560 神经胶质瘤细胞中,SD-208 增加免疫原性,同时阻断组成型、TGF-β 诱发和细胞生长 [1]。在体外,SD-208 通过阻断 TGF-β 诱导的 Smad2 和 Smad3 磷酸化来促进迁移、侵袭和上皮间质转分化 [2]。此外,SD-208 消除了 TGF-β 对体外新生内膜平滑肌样细胞 (SMLC) 迁移和增殖的刺激影响[3]。
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体内研究 (In Vivo) |
使用 SD-208(1 mg/mL,口服)治疗时,携带 SMA-560 神经胶质瘤的小鼠的中位生存期显着延长[1]。 SD-208(60 mg/kg/d,口服)可防止同基因 129S1 小鼠中原发性 R3T 肿瘤的形成,并减少肺转移的数量和大小[2]。 SD-208在小鼠同种异体主动脉移植模型中成功抑制移植动脉硬化(TA)内膜增生的发展[3]。
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动物实验 |
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参考文献 |
[1]. Uhl M, et al. SD-208, a novel transforming growth factor beta receptor I kinase inhibitor, inhibits growth and invasiveness and enhances immunogenicity of murine and human glioma cells in vitro and in vivo. Cancer Res. 2004 Nov 1;64(21):7954-61.
[2]. Ge R, et al. Inhibition of growth and metastasis of mouse mammary carcinoma by selective inhibitor of transforming growth factor-beta type I receptor kinase in vivo. Clin Cancer Res. 2006 Jul 15;12(14 Pt 1):4315-30. [3]. Sun Y, et al. Inhibition of intimal hyperplasia in murine aortic allografts by the oral administration of the transforming growth factor-beta receptor I kinase inhibitor SD-208. J Heart Lung Transplant. 2014 Jun;33(6):654-61 |
分子式 |
C17H10CLFN6
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分子量 |
352.75
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CAS号 |
627536-09-8
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相关CAS号 |
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SMILES |
FC1=CC=C(Cl)C=C1C2=NC(NC3=CC=NC=C3)=C4N=CC=NC4=N2
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化学名 |
2-(5-chloro-2-fluorophenyl)-N-4-pyridinyl-4-pteridinamine
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别名 |
SD-208; SD 208; TGF-β RI Kinase Inhibitor V; SD208;
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
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溶解度 (体内) |
Solubility in Formulation 1: 0.91 mg/mL (2.58 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 9.1 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 0.91 mg/mL (2.58 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 9.1 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.91 mg/mL (2.58 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1% methylcellulose:8 mg/mL 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 2.8349 mL | 14.1743 mL | 28.3487 mL | |
5 mM | 0.5670 mL | 2.8349 mL | 5.6697 mL | |
10 mM | 0.2835 mL | 1.4174 mL | 2.8349 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
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 ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
A,effects of TβRI kinase inhibitor on anchorage-dependent growth.Clin Cancer Res.2006 Jul 15;12(14 Pt 1):4315-30. th> |
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Effects of SD-208 on R3T and 4T1 mammary carcinomasin vivo.Clin Cancer Res.2006 Jul 15;12(14 Pt 1):4315-30. td> |
Mechanisms of action of SD-208in vivo.Clin Cancer Res.2006 Jul 15;12(14 Pt 1):4315-30. td> |