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| 10mg |
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| 25mg |
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Purity: ≥98%
NVP-ADW742 (also known as ADW-742; ADW 742; GSK552602A; GSK-552602A) is a novel, potent and selective IGF-1R inhibitor with potential antitumor activity. Its IC50 value for IGF-1R inhibition is 0.17 μM. When MM-1S-Luc+ human MM cells are injected into male SCID/NOD mice, it shows outstanding in vivo antitumor efficacy.
| Targets |
IGF-1R (GI50 = 0.17 μM); InsR (IC50 = 2.8 μM)
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
The 96-well "Capture ELISAs" assay is used to determine the IC50 value for the effect of NVP-ADW742 on the autophosphorylation of IGF-1R at the cellular level in the presence of increasing concentrations of NVP-ADW742. NWT-21 cells are, in short, seeded into 96-well tissue culture plates in complete growth medium, grown to 70–80% confluency, and then starved in 0.5% FCS medium for a duration of 24 hours. Next, the cells are treated with NVP-ADW742 for 90 minutes, and then they are stimulated for 10 minutes at 37 °C with 10 ng/mL of IGF-I. The cells are then lysed at 4 °C using 50 μL/well RIPA-buffer (50 mM Tris-HCl, pH 7.2, 120 mM NaCl, 1 mM EDTA, 6 mM EGTA, 1% NP-40, 20 mM NaF, 1 mM benzamidine, 15 mM sodium pyrophosphate, 1 mM PMSF, and 0.5 mM Na3VO4) after being rinsed twice with ice-cold PBS. Following that, the lysates from each experiment are put onto black ELISA plates that have been coated with IGF-1R-specific capture antibodies. Following antibody capture, lysates are combined with 40 μL of anti-phosphotyrosine Ab (PY20(AP)) labeled with alkaline phosphatase (AP) and diluted to 0.2 μg/mL in RIPA buffer. The mixture is then incubated for an additional night at 4 °C. The luminescence of the luminescent AP-substrate CDPStar RTU with Emerald II (90 μL/well) is measured using a Packard Top Count Scintillation Counter following washing (PBST) and 45 minutes at room temperature.
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| Cell Assay |
For 48 hours, cells are exposed to different concentrations of NVP-ADW742, either with or without serum. The MTT assay is utilized to analyze cell survival.
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| Animal Protocol |
Male SCID/NOD mice injected i.v. with MM-1S-Luc+ human MM cells
10 mg/kg twice daily Injection i.p. or oral gavage |
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| References |
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| Molecular Formula |
C28H31N5O
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| Molecular Weight |
453.58
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| Exact Mass |
453.252
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| Elemental Analysis |
C, 74.14; H, 6.89; N, 15.44; O, 3.53
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| CAS # |
475488-23-4
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| Related CAS # |
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| PubChem CID |
9825149
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| Appearance |
white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
677.5±55.0 °C at 760 mmHg
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| Flash Point |
363.5±31.5 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.699
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| LogP |
5.23
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
34
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| Complexity |
645
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| Defined Atom Stereocenter Count |
0
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| SMILES |
NC1=C2C(N(C=C2C3=CC=CC(OCC4=CC=CC=C4)=C3)[C@H]5C[C@@H](C5)CN6CCCC6)=NC=N1
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| InChi Key |
LSFLAQVDISHMNB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H31N5O/c29-27-26-25(22-9-6-10-24(15-22)34-18-20-7-2-1-3-8-20)17-33(28(26)31-19-30-27)23-13-21(14-23)16-32-11-4-5-12-32/h1-3,6-10,15,17,19,21,23H,4-5,11-14,16,18H2,(H2,29,30,31)
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| Chemical Name |
5-(3-phenylmethoxyphenyl)-7-[3-(pyrrolidin-1-ylmethyl)cyclobutyl]pyrrolo[2,3-d]pyrimidin-4-amine
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.92 mg/mL (4.23 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 19.2 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1.92 mg/mL (4.23 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 19.2 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.92 mg/mL (4.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2047 mL | 11.0234 mL | 22.0468 mL | |
| 5 mM | 0.4409 mL | 2.2047 mL | 4.4094 mL | |
| 10 mM | 0.2205 mL | 1.1023 mL | 2.2047 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
In vivo antitumor activity of the selective IGF-1R kinase inhibitor NVP-ADW742. Cancer Cell. 2004 Mar;5(3):221-30. |
IGF-1R inhibition sensitizes tumor cells to other anticancer therapies in vitro and in vivo. Cancer Cell. 2004 Mar;5(3):221-30. |
IGF-1R inhibition overcomes the protective effects conferred to MM tumor cells by their local bone microenvironment. Cancer Cell. 2004 Mar;5(3):221-30. |
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