OSI-930
(Synonyms: 噻尔非尼) 目录号 : GC14957
A dual inhibitor of Kit and VEGFR2
Cas No.:728033-96-3
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
OSI-930 is a novel, potent inhibitor of Flt1, kinase insert domain receptor (KDR), CSF-1R, Lck, c-Raf and activated receptor tyrosine kinases Kit with IC50 values of 8, 9, 15, 22, 41 and 80 nM, respectively [1].
OSI-930 has been demonstrated to inhibit proliferation and induce apoptosis in the HMC-1 cell line which is highly dependent on Kit signaling for survival. On the contrary, OSI-930 revealed no growth inhibition of COLO-205 cell line under normal culture conditions [1].
OSI-930 has shown to time- and concentration-dependently inactivate P450 3A4. Additionally, OSI-930 could reduce CO difference spectra of P450 3A4 [2].
References:
[1] Garton AJ1, Crew AP, Franklin M, Cooke AR, Wynne GM, Castaldo L, Kahler J, Winski SL, Franks A, Brown EN, Bittner MA, Keily JF, Briner P, Hidden C, Srebernak MC, Pirrit C, O'Connor M, Chan A, Vulevic B,Henninger D, Hart K, Sennello R, Li AH, Zhang T, Richardson F, Emerson DL, Castelhano AL, Arnold LD,Gibson NW. OSI-930: a novel selective inhibitor of Kit and kinase insert domain receptor tyrosine kinases with antitumor activity in mouse xenograft models. Cancer Res. 2006 Jan 15;66(2):1015-24.
[2] Lin HL1, Zhang H, Medower C, Hollenberg PF, Johnson WW. Inactivation of cytochrome P450 (P450) 3A4 but not P450 3A5 by OSI-930, a thiophene-containing anticancer drug. Drug Metab Dispos. 2011 Feb;39(2):345-50.
| Cas No. | 728033-96-3 | SDF | |
| 别名 | 噻尔非尼 | ||
| 化学名 | 3-(quinolin-4-ylmethylamino)-N-[4-(trifluoromethoxy)phenyl]thiophene-2-carboxamide | ||
| Canonical SMILES | C1=CC=C2C(=C1)C(=CC=N2)CNC3=C(SC=C3)C(=O)NC4=CC=C(C=C4)OC(F)(F)F | ||
| 分子式 | C22H16F3N3O2S | 分子量 | 443.44 |
| 溶解度 | ≥ 22.15mg/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 | 2.2551 mL | 11.2755 mL | 22.551 mL |
| 5 mM | 0.451 mL | 2.2551 mL | 4.5102 mL |
| 10 mM | 0.2255 mL | 1.1275 mL | 2.2551 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。