Toceranib phosphate
(Synonyms: 托西尼布磷酸盐,SU11654 phosphate; PHA 291639E phosphate) 目录号 : GC37808
A multi-targeted receptor tyrosine kinase inhibitor
Cas No.:874819-74-6
Sample solution is provided at 25 µL, 10mM.
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Toceranib is a small molecule, multi-targeted receptor tyrosine kinase inhibitor that is structurally related to sunitinib .1 It potently inhibits signaling through VEGFR, FGFR, PDGFR, and Kit.1 Moveover, toceranib blocks the autophosphorylation of both wild type and mutant forms of Kit in response to stem cell factor, resulting in cell death.1 It is active in vivo and is commonly used against solid tumors in dogs.2,3
1.Liao, A.T., Chien, M.B., Shenoy, N., et al.Inhibition of constitutively active forms of mutant kit by multitargeted indolinone tyrosine kinase inhibitorsBlood100(2)585-593(2002) 2.London, C., Mathie, T., Stingle, N., et al.Preliminary evidence for biologic activity of toceranib phosphate (Palladiar) in solid tumoursVet. Comp. Oncol.10(3)194-205(2012) 3.Ranieri, G., Gadaleta, C.D., Patruno, R., et al.A model of study for human cancer: Spontaneous occurring tumors in dogs. Biological features and translation for new anticancer therapiesCrit. Rev. Oncol. Hematol.88187-197(2013)
Cell experiment: | The c-kit mutant canine C2 mastocytoma cell line, derived from a spontaneously occurring cutaneous mast cell tumors (MCTs), is used as the parental cell line. Cells are propagated in RPMI 1640 supplemented with 2 mM L-glutamine, 10% FBS, 100 g/mL Streptomycin, and 100 U/mL Penicillin in a 37°C incubator under a humidified atmosphere of 5% CO2. Toceranib-resistant C2 cells are selected by growing C2 cells in concentrations of Toceranib ranging from 0.02 uM to 0.3 uM and increasing in 0.025-0.05 uM increments. Three independent, Toceranib -resistant sublines are established over a period of 7 months[2]. |
Animal experiment: | Dogs[3]Fifteen client-owned dogs with advanced tumors are used. Dogs receive Toceranib at 2.75 mg/kg once every other day. After 2 weeks, oral cyclophosphamide (CYC) is added at 15 mg/m2 daily. Numbers of Treg and lymphocyte subsets are measured in blood by flow cytometry during the 8-week study period. Serum concentrations of IFN-γ are measured by ELISA. |
References: [1]. London CA, et al. Phase I dose-escalating study of SU11654, a small molecule receptor tyrosine kinase inhibitor, in dogs with spontaneous malignancies. Clin Cancer Res. 2003 Jul;9(7):2755-68. | |
| Cas No. | 874819-74-6 | SDF | |
| 别名 | 托西尼布磷酸盐,SU11654 phosphate; PHA 291639E phosphate | ||
| Canonical SMILES | O=C(NCCN1CCCC1)C2=C(NC(/C=C3C(NC4=C\3C=C(C=C4)F)=O)=C2C)C.O=P(O)(O)O | ||
| 分子式 | C22H28FN4O6P | 分子量 | 494.45 |
| 溶解度 | DMSO: 2.46 mg/mL (4.98 mM and warming); Water: < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0224 mL | 10.1122 mL | 20.2245 mL |
| 5 mM | 0.4045 mL | 2.0224 mL | 4.0449 mL |
| 10 mM | 0.2022 mL | 1.0112 mL | 2.0224 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet