| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
GSK1904529A (also known as GSK-4529; GSK-1904529A; GSK 4529) is a novel, potent and selective inhibitor of IGF-1R (insulin-like growth factor-1 receptor) and IR (insulin receptor) with potential anticancer activity. It exhibits >100-fold higher selectivity for IGF-1R/InsR than Akt1/2, Aurora A/B, B-Raf, CDK2, EGFR, and so on. In cell-free assays, it inhibits IGF-1R and IR with IC50s of 27 nM and 25 nM, respectively. In tumor-bearing NIH-3T3/LISN mice, GSK1904529A demonstrates exceptional high in vivo antitumor efficacy.
| Targets |
IGF-1R (IC50 = 27 nM); IR (IC50 = 25 nM)
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
In DMSO stock solution, GSK1904529A is dissolved at a concentration of 10 mM. To calculate IC50, proteins tagged with glutathione S-transferase and encoding the intracellular domain of IGF-1R (amino acids 957–1367) and IR (amino acids 979–1382) are expressed by baculoviruses. The process of preincubating the enzyme (at a final concentration of 2.7 μM) in 50 mM HEPES (pH 7.5), 10 mM MgCl2, 0.1 mg/mL bovine serum albumin, and 2 mM ATP activates kinases. Distilled in DMSO, 100 nL/well of GSK1904529A is poured into the assay plates. Included kinase reactions (10 μL) The following ingredients are included: 500 nM substrate peptide (biotin-aminohexylAEEEEYMMMMAKKKK-NH2; QPC), 3 mM DTT, 0.1 mg/mL bovine serum albumin, 1 mM CHAPS, 10 mM MgCl2, 10 μM ATP, and 0.5 nM activated enzyme. After an hour at room temperature with 33 μM EDTA, reactions are terminated. Time-resolved fluorescence resonance energy transfer using 7 nM streptavidin Surelight allophycocyanin and 1 nM europium-conjugated phosphotyrosine antibodies is used to measure phosphorylation of peptides. A multilabel reader reads plates.
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| Cell Assay |
In 96-well plates, cells are seeded, allowed to grow overnight at 37 °C, and then exposed to different concentrations of GSK1904529A for a full 72 hours. On collagen-coated 96-well tissue culture plates, cells are seeded for the NIH-3T3/LISN and given a 24-hour window to adhere. Serum-free medium is used in place of the tissue culture medium, and the cells are treated with either DMSO or GSK1904529A for two hours. Following the addition of IGF-I (30 ng/mL), the cells are incubated for 72 hours at 37 °C. The CellTiter-Glo Luminescent Cell Viability Assay is used to quantify the proliferation of cells. The IC50 values are established.
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| Animal Protocol |
NIH-3T3/LISN, COLO 205, HT29, and BxPC3 cells are implanted s.c. into the right flank of 8- to 10-wk-old female nu/nu CD-1athymic mice
~30 mg/kg Orally administered |
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| References |
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| Additional Infomation |
N-(2,6-difluorophenyl)-5-[3-[2-[5-ethyl-2-methoxy-4-[4-(4-methylsulfonyl-1-piperazinyl)-1-piperidinyl]anilino]-4-pyrimidinyl]-2-imidazo[1,2-a]pyridinyl]-2-methoxybenzamide is a member of benzamides.
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| Molecular Formula |
C44H47F2N9O5S
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| Molecular Weight |
851.96
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| Exact Mass |
851.338
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| Elemental Analysis |
C, 62.03; H, 5.56; F, 4.46; N, 14.80; O, 9.39; S, 3.76
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| CAS # |
1089283-49-7
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| Related CAS # |
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| PubChem CID |
25124816
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.672
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| LogP |
4.69
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
61
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| Complexity |
1530
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C([H])=C([H])C([H])=C(C=1C(=C([H])[H])C(C1=C(C([H])=C([H])C(=C1[H])C1=C(C2([H])C([H])=C([H])N=C(C([H])=C2[H])[N+](=C([H])[H])C2=C(C([H])=C(C(=C2[H])C([H])([H])C([H])([H])[H])N2C([H])([H])C([H])([H])C([H])(C([H])([H])C2([H])[H])N2C([H])([H])C([H])([H])N(C(C([H])(C([H])([H])[H])O[H])=O)C([H])([H])C2([H])[H])OC([H])([H])[H])N2C([H])=C([H])C([H])([H])C([H])([H])C2([H])N1[H])OC([H])([H])[H])=O)F
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| InChi Key |
MOSKATHMXWSZTQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C44H47F2N9O5S/c1-5-28-26-35(38(60-3)27-36(28)53-19-15-30(16-20-53)52-21-23-54(24-22-52)61(4,57)58)49-44-47-17-14-34(48-44)42-40(50-39-11-6-7-18-55(39)42)29-12-13-37(59-2)31(25-29)43(56)51-41-32(45)9-8-10-33(41)46/h6-14,17-18,25-27,30H,5,15-16,19-24H2,1-4H3,(H,51,56)(H,47,48,49)
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| Chemical Name |
N-(2,6-difluorophenyl)-5-[3-[2-[5-ethyl-2-methoxy-4-[4-(4-methylsulfonylpiperazin-1-yl)piperidin-1-yl]anilino]pyrimidin-4-yl]imidazo[1,2-a]pyridin-2-yl]-2-methoxybenzamide
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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: ≥ 2.75 mg/mL (3.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1738 mL | 5.8688 mL | 11.7376 mL | |
| 5 mM | 0.2348 mL | 1.1738 mL | 2.3475 mL | |
| 10 mM | 0.1174 mL | 0.5869 mL | 1.1738 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.
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Effect of GSK1904529A on IR phosphorylation and glucose metabolism. Clin Cancer Res. 2009 May 1;15(9):3058-67. |
Effect of GSK1904529A on IGF-IR phosphorylation in vivo. Clin Cancer Res. 2009 May 1;15(9):3058-67. |
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