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。
Rebastinib (Synonyms: DCC-2036) 纯度: 99.91%
Rebastinib (DCC-2036) 是一种口服有效的,非 ATP 竞争性的 Bcr-Abl 抑制剂,作用于 Abl1WT 和 Abl1T315I,IC50 分别为 0.8 nM 和 4 nM,也抑制 SRC,KDR,FLT3 和 Tie-2,低活性作用于c-Kit。
Rebastinib Chemical Structure
CAS No. : 1020172-07-9
规格 | 价格 | 是否有货 | 数量 |
---|---|---|---|
Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥974 | In-stock | |
5 mg | ¥800 | In-stock | |
10 mg | ¥1400 | In-stock | |
50 mg | ¥5100 | In-stock | |
100 mg | 询价 | ||
200 mg | 询价 |
* Please select Quantity before adding items.
Rebastinib 相关产品
•相关化合物库:
- Covalent Screening Library Plus
- Drug Repurposing Compound Library Plus
- 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
- Drug Repurposing Compound Library
- Covalent Screening Library
- Reprogramming Compound Library
- Anti-COVID-19 Compound Library
- Cytoskeleton Compound Library
- Orally Active Compound Library
- Anti-Alzheimer’s Disease Compound Library
- Anti-Pancreatic Cancer Compound Library
- Anti-Blood Cancer Compound Library
- Anti-Parkinson’s Disease Compound Library
- Neurodegenerative Disease-related Compound Library
- Angiogenesis Related Compound Library
- Rare Diseases Drug Library
生物活性 |
Rebastinib (DCC-2036) is an orally active, non-ATP-competitive Bcr-Abl inhibitor for Abl1WT and Abl1T315I with IC50s of 0.8 nM and 4 nM, respectively. Rebastinib also inhibits SRC, KDR, FLT3, and Tie-2, and has low activity to seen towards c-Kit. |
IC50 & Target |
IC50: 0.75±0.11 nM (ABL1WT), 2±0.3 nM (FLT3), 4±0.3 nM (KDR), 6±0.3 nM (TIE2), 34±6 nM (SRC)[1] |
||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
体外研究 (In Vitro) |
Rebastinib potently (IC50 0.82 nM) inhibits u-ABL1native, which is thought to exist predominantly in the inactive type II conformation. In addition, Rebastinib also strongly inhibits p-ABL1native (IC50 2 nM), which more readily adopts an active, Type I conformation[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. |
||||||||||||||||
体内研究 (In Vivo) |
A single dose of Rebastinib (DCC-2036; oral; 100 mg/kg) affords circulating plasma levels that exceeds 12 μM for up to 24 hours, and effectively inhibits BCR-ABL1 signaling for up to 8 hours in Ba/F3-BCR-ABL1T315I leukemia cells isolated from BM and spleen of tumor-bearing mice[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. |
||||||||||||||||
Clinical Trial |
|
||||||||||||||||
分子量 |
553.59 |
||||||||||||||||
Formula |
C30H28FN7O3 |
||||||||||||||||
CAS 号 |
1020172-07-9 |
||||||||||||||||
运输条件 |
Room temperature in continental US; may vary elsewhere. |
||||||||||||||||
储存方式 |
|
||||||||||||||||
溶解性数据 |
In Vitro:
DMSO : 50 mg/mL (90.32 mM; ultrasonic and warming and heat to 80°C) 配制储备液
*
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。 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
|
||||||||||||||||
参考文献 |
|
Cell Assay [1] |
Ba/F3 cells (3×103 cells/well) or primary Ph+ leukemia cells (5×104 cells/well) are plated in triplicate in 96-well plates containing test compounds (e.g., Rebastinib (DCC-2036)). After 72h, viable cells are quantified by resazurin or MTT assay. Results represent an average of at least three independent experiments[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 Administration [1] |
Mice[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. |
参考文献 |
|
所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务