计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥99% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
2-8°C储存,干燥。低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2 , VEGFR3 , PDGFα , and c-Kit inhibitor with IC 50 s of 6 nM, 4 nM, 15 nM and 1 nM, respectively
In Vitro
Telatinib enhances the anticancer activity of ABCG2 substrate anticancer drugs by inhibiting ATP-binding cassette G2 (ABCG2) efflux transporter activity. Co-incubation of ABCG2-overexpressing drug resistant cell lines with Telatinib and ABCG2 substrate anticancer drugs significantly reduces cellular viability, whereas Telatinib alone does not significantly affect drug sensitive and drug resistant cell lines. Telatinib at 1 μM does not significantly alter the expression of ABCG2 in ABCG2-overexpressing cell lines. Telatinib at 1 μM significantly enhances the intracellular accumulation of [ 3 H]-mitoxantrone (MX) in ABCG2-overexpressing cell lines. Telatinib at 1 μM significantly reduces the rate of [ 3 H]-MX efflux from ABCG2-overexpressing cells. Furthermore, Telatinib significantly inhibits ABCG2-mediated transport of [ 3 H]-E₂17βG in ABCG2 overexpressing membrane vesicles. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Telatinib (15 mg/kg; oral dministration; every 2nd and 3rd day; total 12 times; male athymic NCR (nu/nu) nude mice) with Doxorubicin (1.8 mg/kg) significantly decreases the growth rate and tumor size of ABCG2 overexpressing tumors in a xenograft nude mouse model. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male athymic NCR (nu/nu) nude mice (13-15 g, age 4-5 weeks) injected with H460 and H460/MX20 cellsDosage: 15 mg/kg Administration: Oral dministration; every 2nd and 3rd day; total 12 times Result: With Doxorubicin (1.8 mg/kg) significantly decreased the growth rate and tumor size of ABCG2 overexpressing tumors in a xenograft nude mouse model.
Form:Solid
IC50& Target:VEGFR2 6 nM (IC 50 ) VEGFR3 4 nM (IC 50 ) PDGFRα 15 nM (IC 50 ) c-Kit 1 nM (IC 50 )
规格
别名
甲磺酸替拉替尼
规格或纯度
≥99%
英文名称
Telatinib mesylate
生化机理
甲磺酸替拉替尼（Bay 57-9352 mesylate）是一种强效口服活性 VEGFR2、VEGFR3、PDGFα 和 c-Kit 抑制剂，其 IC 50 s 分别为 6 nM、4 nM、15 nM 和 1 nM。
储存条件
2-8°C储存,干燥
运输条件
低温运输
纯度
≥99%
名称和识别符
分子类型
小分子
Smiles
O=C(C1=NC=CC(COC2=NN=C(NC3=CC=C(Cl)C=C3)C4=C2OC=C4)=C1)NC.OS(=O)(C)=O
分子量
505.93
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 250 mg/mL (494.14 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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