Telatinib (BAY 57-9352)
(Synonyms: 替拉替尼,BAY 579352;BAY 57 9352) 目录号 : GC11763
A multi-kinase inhibitor
Cas No.:332012-40-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kinase experiment: | The vanadate (Vi)-sensitive ATPase activity of ABCG2 in the membrane of High Five insect cells is measured. Briefly, membrane (2 μg/0.06 mL) are incubated in ATPase assay buffer with or without 0.4 mM vanadate at 37°C for 5 min and then incubated with varying concentrations of telatinib at 37°C for 5 min. The ATPase reaction is started by the addition of 4 mM Mg-ATP. After incubating at 37°C for 10 min, the reactions are stopped by adding 0.05 mL of 10% SDS solution. The liberated inorganic phosphate is measured[4]. |
Animal experiment: | Mice: The mice are randomized into four groups and treated with one of the following regimens: (a) vehicle (10% N-methyl-pyrrolidinone, 90% polyethylene glycol 300) (q3d×6), (b) DOX (1.8 mg/kg, i.p., q3d×6), (c) telatinib dissolved in 10% N-methyl-pyrrolidinone, 90% polyethylene glycol 300 (15 mg/kg, p.o., every 2nd and 3rd day; total 12 times), and (d) DOX (1.8 mg/kg, i.p., q3d×6) + telatinib (15 mg/kg, p.o., every 2nd and 3rd day, given 1 h before giving DOX; total 12 times). DOX for injection is prepared by dissolving in saline. Tumor volume is measured using calipers and body weights are recorded[4]. |
References: [1]. Steeghs N, et al. Hypertension and rarefaction during treatment with telatinib, a small molecule angiogenesis inhibitor. Clin Cancer Res. 2008 Jun 1;14(11):3470-6. | |
Telatinib (BAY 57-9352) is a selective inhibitor of VEGFR2, VEGFR3, c-Kit and PDGFRα with IC50 value of 6 nM, 4 nM, 1 nM and 15 nM, respectively [1].
Vascular endothelial growth factor receptor (VEGFR) is the receptor of VEGF and plays an important role in stimulating vasculogenesis and angiogenesis. Platelet-derived growth factor (PDGF) is a member of growth factors and involves in blood vessel formation. C-Kit is the receptor of a growth factor. Many studies have shown that abnormal of VEGFR, c-Kit and PDGFR are correlated with a variety of tumors [1, 2, 3].
Telatinib is a potent VEGFR2/3, c-Kit and PDGFRα inhibitor. When tested with a panel of tumor cell lines (MDA-MB-231 breast caicinoma, Colo-205 colon carcinoma, DLD-1 colon carcinoma and H460 non-small cell lung carcinoma), Telatinib treatment exhibited inhibition on VEGFR-2 autophosphorylation and PDGF-βwhich involved in the angiogenic process [2].
Telatinib has been used in clinical trails to a variety of cancers treatment and has achieved promising results [2-4].
It is also reported that Telatinib restores tumor cells sensitivity to anticancer drugs and significantly reduced cellular viability by inhibiting ABCG2 expression [3].
References:
[1]. Steeghs, N., et al., Hypertension and rarefaction during treatment with telatinib, a small molecule angiogenesis inhibitor. Clin Cancer Res, 2008. 14(11): p. 3470-6.
[2]. Strumberg, D., et al., Phase I dose escalation study of telatinib (BAY 57-9352) in patients with advanced solid tumours. Br J Cancer, 2008. 99(10): p. 1579-85.
[3]. Sodani, K., et al., Telatinib reverses chemotherapeutic multidrug resistance mediated by ABCG2 efflux transporter in vitro and in vivo. Biochem Pharmacol, 2014. 89(1): p. 52-61.
[4]. Eskens, F.A., et al., Phase I dose escalation study of telatinib, a tyrosine kinase inhibitor of vascular endothelial growth factor receptor 2 and 3, platelet-derived growth factor receptor beta, and c-Kit, in patients with advanced or metastatic solid tumors. J Clin Oncol, 2009. 27(25): p. 4169-76.
| Cas No. | 332012-40-5 | SDF | |
| 别名 | 替拉替尼,BAY 579352;BAY 57 9352 | ||
| 化学名 | 4-[[4-(4-chloroanilino)furo[2,3-d]pyridazin-7-yl]oxymethyl]-N-methylpyridine-2-carboxamide | ||
| Canonical SMILES | CNC(=O)C1=NC=CC(=C1)COC2=NN=C(C3=C2OC=C3)NC4=CC=C(C=C4)Cl | ||
| 分子式 | C20H16ClN5O3 | 分子量 | 409.83 |
| 溶解度 | ≥ 20.5mg/mL in DMSO | 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 | 2.44 mL | 12.2002 mL | 24.4004 mL |
| 5 mM | 0.488 mL | 2.44 mL | 4.8801 mL |
| 10 mM | 0.244 mL | 1.22 mL | 2.44 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。