NVP-ADW742 (Synonyms: ADW742, GSK552602A) |
Catalog No.GC14310
One-Click Copy Product Info
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NVP-ADW742(ADW742)는 IC50이 0.17μM인 경구 활성 선택적 IGF-1R 티로신 키나제 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 475488-23-4
Sample solution is provided at 25 µL, 10mM.
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NVP-ADW742 is a novel inhibitor of IFG-1receptor (IGF-1R) kinase with the IC50 value of 0.17μM [1].
NVP-ADW742 has shown above 16-fold effective function against IGF-1R than insulin receptor (InsR). Furthermore, NVP-ADW742 has also been reported to inhibit other kinases , with the IC50 values of ＞10μM for HER2, PDGFR, VEGFR-2, or Bcr-Abl p210, and the IC50 values ＞5μM for c-Kit [1]. Besides, NVP-ADW742 combined with etoposide and carboplatin has been reported to inhibit cell growth and induce cytotoxicity by MTT assay using the small cell lung cancer (SCLC), including H526, H146, WBA and H209 cell lines. In addition, NVP-ADW742 has been revealed to completely inhibit the expression of VEGF mRNA which induced by IGF-I in H526 cells [2].
References:
[1] Mitsiades CS1, Mitsiades NS, McMullan CJ, Poulaki V, Shringarpure R, Akiyama M, Hideshima T, Chauhan D, Joseph M, Libermann TA, García-Echeverría C, Pearson MA, Hofmann F, Anderson KC, Kung AL. Inhibition of the insulin-like growth factor receptor-1 tyrosine kinase activity as a therapeutic strategy for multiple myeloma, other hematologic malignancies, and solid tumors . Cancer Cell. 2004 Mar; 5(3):221-30.
[2]Warshamana-Greene GS1, Litz J, Buchdunger E, García-Echeverría C, Hofmann F, Krystal GW. The insulin-like growth factor-I receptor kinase inhibitor, NVP-ADW742, sensitizes small cell lung cancer cell lines to the effects of chemotherapy. Clin Cancer Res. 2005 Feb 15;11(4):1563-71.
| Cas No. | 475488-23-4 | SDF | |
| Synonyms | ADW742, GSK552602A | ||
| Chemical Name | 5-(3-phenylmethoxyphenyl)-7-[3-(pyrrolidin-1-ylmethyl)cyclobutyl]pyrrolo[2,3-d]pyrimidin-4-amine | ||
| Canonical SMILES | C1CCN(C1)CC2CC(C2)N3C=C(C4=C3N=CN=C4N)C5=CC(=CC=C5)OCC6=CC=CC=C6 | ||
| Formula | C28H31N5O | M.Wt | 453.58 |
| Solubility | DMF: 30 mg/mL,DMSO: 30 mg/mL,Ethanol: 30 mg/mL,Ethanol:PBS (pH 7.2) (1:10): 0.09 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. |
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| 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 | 2.2047 mL | 11.0234 mL | 22.0468 mL |
| 5 mM | 440.9 μL | 2.2047 mL | 4.4094 mL |
| 10 mM | 220.5 μL | 1.1023 mL | 2.2047 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 saline, 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% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)