CP-673451 |
| Catalog No.GC12980 |
PDGFRα/β inhibitor,potent and selective
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 343787-29-1
Sample solution is provided at 25 µL, 10mM.
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CP-673451 is a potent inhibitor of PDGFR with IC50 value of 10nM and 1nM for PDGFR-α and PDGFR-β, respectively [1].
CP-673451 is an ATP-competitive inhibitor and is investigated to treat for cancer. It is highly selective against PDGFR-α and PDGFR-β over a variety of other kinases such as VEGFR-1, VEGFR-2, Lck, TIE-2 and EGFR. In PAE-β cells, CP-673451 inhibits PDGFR-β with IC50 value of 6.4nM. CP-673451 also inhibits c-kit with IC50 value of 1.1μM in H526 cells. In rat C6 glioblastoma xenograft models, a single oral dose of 50mg/kg CP-673451 reduces > 50% phosphorylation of PDGFR-β for 4 hours. In addition, CP-673451 is found to inhibit PDGF-BB-induced angiogenesis in a sponge angiogenesis model. Furthermore, CP-673451 inhibits the tumor growth in Colo205, LS174T, H460, and U87MG xenograft models. It also reduces the microvessel density of Colo205 xenografts [1].
References:
[1] Roberts W G, Whalen P M, Soderstrom E, et al. Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451. Cancer research, 2005, 65(3): 957-966.
| Cell experiment [1]: | |
|
Cell lines |
PAE-β cells and H526 cells |
|
Preparation method |
The solubility of this compound in DMSO is > 20.9 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
|
Reacting condition |
0 nM ~ 3 mM |
|
Applications |
In PAE-β cells, CP-673451 inhibited PDGFR-β in a dose-dependent manner, with the IC50 value of 6.4nM. CP-673451 also inhibited c-kit in H526 cells, with the IC50 value of 1.1 μM. However, CP-673451 was > 180× selective for PDGFR-β compared with c-kit in H526 cells. |
| Animal experiment [1]: | |
|
Animal models |
Mouse sponge angiogenesis model |
|
Dosage form |
3, 10 or 30 mg/kg; p.o.; q.d., for 5 days |
|
Applications |
CP-673451 (3, 10 or 30 mg/kg; p.o.; q.d., for 5 days) inhibited PDGF-BB-induced angiogenesis by 70 ~ 90%. Corresponding Cmax plasma concentrations after the last dose were 5.5 ~ 419 ng/mL. Besides, CP-673451 showed selective inhibition on PDGF-BB-induced angiogenesis over VEGF- or bFGF-induced angiogenesis (no inhibition observed). |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Roberts W G, Whalen P M, Soderstrom E, et al. Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451. Cancer research, 2005, 65(3): 957-966. | |
| Cas No. | 343787-29-1 | SDF | |
| Chemical Name | 1-[2-[5-(2-methoxyethoxy)benzimidazol-1-yl]quinolin-8-yl]piperidin-4-amine | ||
| Canonical SMILES | COCCOC1=CC2=C(C=C1)N(C=N2)C3=NC4=C(C=CC=C4N5CCC(CC5)N)C=C3 | ||
| Formula | C24H27N5O2 | M.Wt | 417.52 |
| Solubility | ≥ 20.9mg/mL in DMSO | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3951 mL | 11.9755 mL | 23.9509 mL |
| 5 mM | 0.479 mL | 2.3951 mL | 4.7902 mL |
| 10 mM | 0.2395 mL | 1.1975 mL | 2.3951 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)
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