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Purity: ≥98%
GSK1838705A (GSK-1838705A) is a novel, potent and reversible small-molecule IGF-1R inhibitor with potential anticancer activity. IGF-1R is inhibited with an IC50 of 2.0 nM. GSK1838705A shows little activity against other protein kinases and has IC50s of 1.6 nM and 0.5 nM, respectively, making it moderately potent against IR and ALK.
| Targets |
ALK (IC50 = 0.5 nM); Insulin Receptor (IC50 = 1.6 nM); IGF-1R (IC50 = 2 nM)
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| Enzyme Assay |
The intracellular domains of IGF-1R (amino acids 957–1367) and IR (amino acids 979–1382) encoded by glutathione S-transferase-tagged baculovirus-expressed proteins are utilized to determine IC50s using a homogeneous time-resolved fluorescence assay. To determine appKi, IR kinases and activated IGF-1R are used in a filter binding assay. GSK1838705A's expanded kinase-selectivity profiling is done by running the compound through the KinaseProfiler panel.
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| Cell Assay |
In 96-well plates, cells are seeded, allowed to grow overnight at 37°C, and then exposed to either DMSO or GSK1838705A for a full 72 hours. Cells are plated on collagen-coated 96-well tissue culture plates for the NIH-3T3/LISN proliferation assays, and they are left to adhere for twenty-four hours. After switching out the medium for serum-free medium, the cells are given a two-hour treatment with GSK1838705A. After adding 30 ng/mL of IGF-I, the cells are incubated for 72 hours. The CellTiter-Glo Luminescent Cell Viability Assay is used to quantify the proliferation of cells. A four-parameter curve fit software program is used to calculate IC50s from cytotoxicity curves.
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| Animal Protocol |
Mice: Female nu/nu CD-1 or SCID mice, ages 8 to 12 weeks, have their right flanks surgically implanted with exponentially growing cells. Mice receive a p.o. dose of GSK1838705A, the formulating vehicle. Twice a week, mice are weighed and their tumors measured with calipers. Calculations are made for tumor volumes.
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| References |
| Molecular Formula |
C27H29FN8O3
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| Molecular Weight |
532.57
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| Exact Mass |
532.23332757
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| Elemental Analysis |
C, 60.89; H, 5.49; F, 3.57; N, 21.04; O, 9.01
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| CAS # |
1116235-97-2
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| Related CAS # |
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| Appearance |
white solid powder
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| SMILES |
CNC(=O)C1=C(C=CC=C1F)NC2=NC(=NC3=C2C=CN3)NC4=C(C=C5CCN(C5=C4)C(=O)CN(C)C)OC
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| InChi Key |
HZTYDQRUAWIZRE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H29FN8O3/c1-29-26(38)23-17(28)6-5-7-18(23)31-25-16-8-10-30-24(16)33-27(34-25)32-19-13-20-15(12-21(19)39-4)9-11-36(20)22(37)14-35(2)3/h5-8,10,12-13H,9,11,14H2,1-4H3,(H,29,38)(H3,30,31,32,33,34)
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| Chemical Name |
2-[[2-[[1-[2-(dimethylamino)acetyl]-5-methoxy-2,3-dihydroindol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methylbenzamide
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| Synonyms |
GSK-1838705A; GSK 1838705A; GSK1838705A
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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) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8777 mL | 9.3884 mL | 18.7769 mL | |
| 5 mM | 0.3755 mL | 1.8777 mL | 3.7554 mL | |
| 10 mM | 0.1878 mL | 0.9388 mL | 1.8777 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.
Pharmacodynamics of GSK1838705A and antitumor activity. A, effect of GSK1838705A on IGF-IR phosphorylation in vivo. Mol Cancer Ther. 2009 Oct;8(10):2811-20. |
Effect of GSK1838705A on IR phosphorylation and metabolic end points in vivo. Mol Cancer Ther. 2009 Oct;8(10):2811-20. |
Antitumor efficacy of GSK1838705A in ALK-dependent tumor xenografts. Mol Cancer Ther. 2009 Oct;8(10):2811-20. |
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