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JI-101

产品编号: DC10123 Featured
JI-101
结构式
900573-88-8
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中国地区超过5000个高品质化合物库存
应用领域
JI-101是有口服活性的有抗癌活性的多靶点激酶抑制剂，可抑制 VEGFR2，PDGFRβ 和 EphB4。
化学性质生物活性化合物的使用COA & MSDS相关产品产品说明书
Cas No.: 900573-88-8
名称:
别名: JI101,JI 101
SMILES: COC1=C(C=C(C=C1)Br)NC(=O)NC2=CC=CC3=C2C=CN3CC4=CC(=NC=C4)N
分子式: C22H20BrN5O2
分子量: 466.33
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: JI-101 is an oral multi-kinase inhibitor that targets vascular endothelial growth factor receptor type 2 (VEGFR-2), platelet derived growth factor receptor β (PDGFR-β), and ephrin type-B receptor 4 (EphB4). JI-101 inhibits angiogenesis, and subsequently tumor growth. In vitro :Caco-2 human intestinal epithelial cells were plated in 24-Transwell dual chamber plates (cell density of 500 000 cells/cm2 on day-1). The permeability studies were conducted with the monolayers cultured for 20-23 days in culture. The integrity of each Caco-2 cell monolayer was certified by trans-epithelial electrical resistance (TEER) test (pre-experiment) and by determining the permeability of reference compounds3H-propranolol (high permeability) and 3H-mannitol (low permeability). In addition, the reference substrate 3H-vinblastine was included as a positive control P-gp substrate. The concentration of JI-101 used in the assay was 10 and 100 uM. All the stocks were made in DMSO and the final concentration of DMSO in spiking solution was 0.5%. in vivo: For oral administration JI-101 was formulated as a suspension with 20 μL of Tween-80 and 0.5% methyl cellulose. Pharmacokinetics and bioavailability assessment of JI-101 were evaluated in a preliminary parallel-group study in male S.D. rats. Four rats (195-210 g) per route received JI-101 at a dose of 3 and 30 mg/kg for i.v. (via tail vein) and oral dose (by gavage), respectively
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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