AG-370 (Synonyms: NSC 651712) |
| Catalog No.GC11712 |
PDGFR inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 134036-53-6
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
IC50: 20 μM for PDGF receptor kinase in human bone marrow fibroblasts
AG-370 is a tyrphostin PDGFR inhibitor.
Protein tyrosine kinase inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of protein tyrosine kinases. Tyrphostins are a class of antiproliferative agents selectively inhibiting protein tyrosine kinases of key growth factors including epidermal growth factor or platelet-derived growth factor (PDGF) via blocking the phosphorylation of tyrosine residues.
In vitro: Previous study found that AG-370 inhibited PDGF receptor autophosphorylation and the tyrosine phosphorylation of intracellular protein substrates that coprecipitated with the PDGF receptor in digitonin-permeabilized fibroblasts and in intact fibroblasts. When compared with AG18, a potent EGF receptor blocker, AG370 was more efficient in inhibiting PDGF-induced proliferation of fibroblasts and phosphorylation of the intracellular protein substrates. Under the conditions in which AG370 could inhibit PDGF-induced mitogenesis and phosphorylation, AG18 did not alter [125I]PDGF internalization and enhance [125I]PDGF binding. These findings suggested that AG370 might have a therapeutic potential for treatment of diseases involving abnormal cellular proliferation induced by PDGF [1].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Bryckaert, M. C.,Eldor, A.,Fontenay, M., et al. Inhibition of platelet-derived growth factor-induced mitogenesis and tyrosine kinase activity in cultured bone marrow fibroblasts by tyrphostins. Experimental Cell Research 199, 255-261 (1992).
| Cas No. | 134036-53-6 | SDF | |
| Synonyms | NSC 651712 | ||
| Chemical Name | 3-amino-4-(1H-indol-5-ylmethylene)-2-pentenetricarbonitrile | ||
| Canonical SMILES | c12c(ccc(c1)/C=C(\C(=C(\C#N)C#N)N)C#N)[nH]cc2 | ||
| Formula | C15H9N5 | M.Wt | 259.3 |
| Solubility | ≤30mg/ml in DMSO;30mg/ml in dimethyl formamide | 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 | 3.8565 mL | 19.2827 mL | 38.5654 mL |
| 5 mM | 0.7713 mL | 3.8565 mL | 7.7131 mL |
| 10 mM | 0.3857 mL | 1.9283 mL | 3.8565 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *