SKLB1002
目录号 : GC13738
A VEGFR2 inhibitor
Cas No.:1225451-84-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
SKLB1002 is a potent inhibitor of VEGF receptor 2 with IC50 value of 32 nM [1].
VEGF receptor 2 (VEGFR2) is a major receptor for vascular endothelial growth factor (VEGF) and plays an important role in angiogenesis and VEGF-stimulated proliferation, migration, and sprouting of cultured endothelial cells [1].
SKLB1002 is a potent VEGFR2 inhibitor. In human umbilical vein endothelial cells (HUVEC), SKLB1002 significantly inhibited VEGF-induced HUVEC proliferation with IC50 value of 11.9 μM. Also, SKLB1002 inhibited HUVEC migration, invasion and tube formation in a dose-dependent way. SKLB1002 (10 μM) significantly inhibited VEGF-induced phosphorylation of VEGFR2, ERK, Src and FAK [1].
In zebrafish embryos, SKLB1002 (2.5 μM) significantly inhibited the growth of intersegmental vessels. In mice bearing SW620 or HepG2 xenografts, SKLB1002 (100 mg/kg) significantly inhibited tumor volume and inhibited tumor growth by 60%. Also, SKLB1002 reduced the microvessel density [1]. In mice with 4T1 tumor, SKLB1002 significantly reduced the tumor vessel density [2].
References:
[1]. Zhang S, Cao Z, Tian H, et al. SKLB1002, a novel potent inhibitor of VEGF receptor 2 signaling, inhibits angiogenesis and tumor growth in vivo. Clin Cancer Res, 2011, 17(13): 4439-4450.
[2]. Shen G, Li Y, Du T, et al. SKLB1002, a novel inhibitor of VEGF receptor 2 signaling, induces vascular normalization to improve systemically administered chemotherapy efficacy. Neoplasma, 2012, 59(5): 486-493.
| Cas No. | 1225451-84-2 | SDF | |
| 化学名 | 2-(6,7-dimethoxyquinazolin-4-yl)sulfanyl-5-methyl-1,3,4-thiadiazole | ||
| Canonical SMILES | CC1=NN=C(S1)SC2=NC=NC3=CC(=C(C=C32)OC)OC | ||
| 分子式 | C13H12N4O2S2 | 分子量 | 320.39 |
| 溶解度 | ≥ 8mg/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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.1212 mL | 15.606 mL | 31.212 mL |
| 5 mM | 0.6242 mL | 3.1212 mL | 6.2424 mL |
| 10 mM | 0.3121 mL | 1.5606 mL | 3.1212 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。