R1530 |
| رقم الكتالوجGC12857 |
A multi-kinase inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 882531-87-5
Sample solution is provided at 25 µL, 10mM.
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R1530 is a potent and orally active inhibitor of mitosis/angiogenesis [1].
Mitosis is a part of the cell cycle process by which chromosomes in a cell nucleus are separated into two identical sets with each in its own nucleus. Angiogenesis refers to the growth of new blood vessels and is an essential component in the progression and metastasis of tumors [1].
R1530 showed potent inhibitory activities against cyclin-dependent kinases, such as CDK2 and CDK4, and angiogenesis-related growth factor receptor, such as KDR, FGFr, PDGFr, and EGFr [1]. In a series of human tumor cell lines, R1530 inhibited the growth of cells with IC50 values ranging from 0.22 to 3.43 μM. Also, R1530 strongly inhibited human umbilical vein endothelial cells (HUVEC) growth driven by VEGF or bFGF with IC50 values of 49 nM and 118 nM, respectively [2].
In nude mice bearing human H460 tumor xenografts, R1530 (3 to 25 mg/kg, orally twice a day, 20 days) inhibited tumor growth in a dose-dependent way. R1530 (the 25 mg/kg dose) reduced tumor size by 58% in average [3].
References:
[1]. Liu JJ, Higgins B, Ju G, et al. Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors. ACS Med Chem Lett, 2013, 4(2): 259-263.
[2]. Kolinsky K, Tovar C, Zhang YE, et al. Preclinical evaluation of the novel multi-targeted agent R1530. Cancer Chemother Pharmacol, 2011, 68(6): 1585-1594.
[3]. Tovar C, Higgins B, Deo D, et al. Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy. Cell Cycle, 2010, 9(16): 3364-3375.
| Cas No. | 882531-87-5 | SDF | |
| Chemical Name | 5-(2-chlorophenyl)-7-fluoro-8-methoxy-3-methyl-1,2-dihydropyrazolo[3,4-b][1,4]benzodiazepine | ||
| Canonical SMILES | CC1=C2C(=NC3=CC(=C(C=C3C(=N2)C4=CC=CC=C4Cl)F)OC)NN1 | ||
| Formula | C18H14ClFN4O | M.Wt | 356.78 |
| الذوبان | DMF: 30 mg/mL,DMSO: 30 mg/mL,DMSO:PBS (pH 7.2) (1:7): 0.12 mg/mL,Ethanol: 20 mg/mL | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8028 mL | 14.0142 mL | 28.0285 mL |
| 5 mM | 560.6 μL | 2.8028 mL | 5.6057 mL |
| 10 mM | 280.3 μL | 1.4014 mL | 2.8028 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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