OSI-930(Synonyms: 噻尔非尼)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

OSI-930 (Synonyms: 噻尔非尼) 纯度: 98.13%

OSI-930 是 Kit，KDR 和 CSF-1R (c-Fms) 的口服有效选择性抑制剂，IC50 分别为 80 nM，9 nM 和 15 nM。OSI-930 还适度抑制 Flt-1，c-Raf 和 Lck，并且对 PDGFRα/β，Flt-3 和 Abl 具有较弱的抑制活性。OSI-930 具有抗肿瘤活性。

OSI-930(Synonyms: 噻尔非尼)

OSI-930 Chemical Structure

CAS No. : 728033-96-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1073 In-stock
2 mg ￥750 In-stock
5 mg ￥1100 In-stock
10 mg ￥1650 In-stock
50 mg ￥5675 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

OSI-930 相关产品

•相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Orally Active Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

OSI-930 is an orally selective inhibitor of Kit, KDR and CSF-1R (c-Fms) with IC50s of 80 nM, 9 nM and 15 nM, respectively. OSI-930 also moderately inhibits Flt-1, c-Raf, Lck and low activity against PDGFRα/β, Flt-3 and Abl. OSI-930 has antitumor activity[1].

IC50 & Target

KDR

9 nM (IC50)

Flt-1

8 nM (IC50)

Kit

80 nM (IC50)

PDGFRβ

6900 nM (IC50)

PDGFRα

3408 nM (IC50)

CSF-1R

15 nM (IC50)

c-Raf

41 nM (IC50)

Flt-3

1303 nM (IC50)

Lck

22 nM (IC50)

Abl

4738 nM (IC50)

体外研究
(In Vitro)

OSI-930 inhibits cell proliferation in the HMC-1 cell line with IC50 of 14 nM but has no significant effect on the growth of COLO-205 cell line that does not express constitutively active mutant receptor tyrosine kinase[1]. OSI-930 induces apoptosis in HMC-1 cell line with an EC50 value of 34 nM[1]. OSI-930 inactivates purified, recombinant cytochrome P450 3A4 with a Ki of 24 μM in a time- and concentration-dependent manner[2]

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

OSI-930 (oral gavage; once a day; 38 days; 200 mg/kg) exhibits potent antitumor activity in a broad range of preclinical xenograft models[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female nu/nu CD-1 mice bearing HMC-1, NCI-SNU-5, COLO-205 and U251 xenograft models[1]
Dosage: 200 mg/kg
Administration: Oral gavage; once a day; 38 days
Result: Showed a significant level of inhibition of Kit, KDR and CSF-1R.

Clinical Trial

分子量

443.44

Formula

C22H16F3N3O2S
CAS 号

728033-96-3
中文名称

噻尔非尼
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (112.75 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2551 mL 11.2755 mL 22.5510 mL
5 mM 0.4510 mL 2.2551 mL 4.5102 mL
10 mM 0.2255 mL 1.1275 mL 2.2551 mL

*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.64 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.64 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.64 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.64 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Garton AJ, et al. 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, 66(2):1015-1024.

    [2]. Lin HL, et al. Inactivation of cytochrome P450 (P450) 3A4 but not P450 3A5 by OSI-930, a thiophene-containing anticancer drug. Drug Metab Dispos. 2011, 39(2), 345-350.

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