Galunisertib (LY2157299)
Modify Date: 2024-01-02 19:45:41
Galunisertib (LY2157299) structure
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Common Name | Galunisertib (LY2157299) | ||
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| CAS Number | 700874-72-2 | Molecular Weight | 369.419 | |
| Density | 1.4±0.1 g/cm3 | Boiling Point | 619.0±55.0 °C at 760 mmHg | |
| Molecular Formula | C22H19N5O | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 328.2±31.5 °C | |
Use of Galunisertib (LY2157299)Galunisertib (LY2157299) is a selective TGF-β receptor inhibitor with an IC50 of 56 nM. |
| Name | 2-(6-methylpyridin-2-yl)-3-(6-aminocarbonylquinolin-4-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole |
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| Synonym | More Synonyms |
| Description | Galunisertib (LY2157299) is a selective TGF-β receptor inhibitor with an IC50 of 56 nM. |
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| Related Catalog | |
| Target |
IC50: 56 nM (TGF-βR)[1] |
| In Vitro | Galunisertib (LY2157299) is a selective ATP-mimetic inhibitor of TGF-β receptor (TβR)-I activation LY2157299 (0.1, 1, 10, and 100 μM) displays a slight dose-dependent potentiation of Sorafenib in SK-Sora, HepG2, and Hep3B cell lines but not in JHH6, SK-HEP1, and HuH7 cell lines[2]. |
| In Vivo | Human xenografts Calu6 (non-small cell lung cancer) and MX1 (breast cancer) are implanted subcutaneously in nude mice. After oral administration of 75 mg/kg, Galunisertib (LY2157299) induces a 70% decrease in pSmad for both types of cell lines. The time at which pSmad recovered 80% of baseline is approximately 6 h after administration[3]. |
| Cell Assay | Cell survival is determined using the MTT assay. The conversion of yellow water-soluble tetrazolium MTT into purple insoluble formazan is catalyzed by mitochondrial dehydrogenases and used to estimate the number of viable cells. In brief, cells are seeded in 96-well tissue culture plates at a density of 2×103 cells/well. After drug exposure, cells are incubated with 0.4 mg/mL MTT for 4 hours at 37°C. After incubation, the supernatant is discarded, insoluble formazan precipitates are dissolved in 0.1 mL of DMSO, and the absorbance is measured at 560 nm by use of a microplate reader. Wells with untreated cells or with drug-containing medium without cells are used as positive and negative controls respectively. For proliferation assay, MTT assay is done daily to determine the number of viable cells in untreated control andGalunisertib (LY2157299) (0.1, 1, 10, and 10 μM)-treated group[2]. |
| Animal Admin | Mice[3] Charles River nude mice (weight 25 mg) are used. Galunisertib (LY2157299) is given orally as a single dose or in a multiple dosing design. The value of the dose levels given in a single dose manner is 10 (n=3), 30 (n=8), 50 (n=26), 75 (n=69), 100 (n=3), 150 (n=21) and 300 (n=3) mg/kg. Animals are sacrificed at the following times: 0.5, 1, 1.5, 2, 4, 8 and 16 h after administration, then the tumor is removed and blood is recovered. In the multiple dosing study, Galunisertib (LY2157299) is administered twice a day (bid) at the dose of 75 mg/kg every 12 h for 20 consecutive days to 31 mice. Animals are sacrificed at 2 h after the last administration at days 10, 15, 20 and 25, and the tumor is removed for pSmad determination and the blood is recovered for determination of drug levels in plasma. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 619.0±55.0 °C at 760 mmHg |
| Molecular Formula | C22H19N5O |
| Molecular Weight | 369.419 |
| Flash Point | 328.2±31.5 °C |
| Exact Mass | 369.158966 |
| PSA | 86.69000 |
| LogP | 1.73 |
| Vapour Pressure | 0.0±1.8 mmHg at 25°C |
| Index of Refraction | 1.751 |
| Storage condition | 2-8°C |
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~64%
Galunisertib (L... CAS#:700874-72-2 |
| Literature: WO2004/48382 A1, ; Page 10 ; |
![METHYL 4-(2-(6-METHYLPYRIDIN-2-YL)-5,6-DIHYDRO-4H-PYRROLO[1,2-B]PYRAZOL-3-YL)QUINOLINE-6-CARBOXYLATE structure](https://www.chemsrc.com/caspic/071/476475-44-2.png)
| Precursor 1 | |
|---|---|
| DownStream 1 | |
![4-[2-(6-methylpyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl]quinoline-6-carboxamide,hydrate structure](https://www.chemsrc.com/caspic/234/924898-09-9.png)
CAS#:924898-09-9| 2-(6-Methyl-pyridin-2-yl)-1-quinoxalin-6-yl-ethanone |
| 4-[2-(6-methylpyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl]quinoline-6-carboxamide |
| 2-(6-methyl-pyridin-2-yl)-3-(6-amido-quinolin-4-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole |
| LY2157299 |
| LY-2157299 |
| LY 2157299 |
| 6-Quinolinecarboxamide, 4-[5,6-dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]- |
| Galunisertib |
| 4-[2-(6-Methyl-2-pyridinyl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-quinolinecarboxamide |
| 6-[2-(6-Methylpyridin-2-yl)-acetyl]quinoxaline |