ChemicalBook > CAS DataBase List > GSK-2256098

GSK-2256098

Product Name: GSK-2256098
CAS No.: 1224887-10-8
Chemical Name: GSK-2256098
Synonyms: CS-2424;GTPL7939;GSK-2256099;GSK-2256098;GSK-2256098, GTPL7939;GSK-2256098;GSK 2256098;FAK inhibitor GS2256098;GSK2256098, 10 mM in DMSO;2-(5-chloro-2-(1-isopropyl-3-methyl-1H-pyrazol-5-ylamino)pyridin-4-ylamino)-N-methoxybenzamide;2-[(5-chloro-2-{[3-methyl-1-(1-methylethyl)-1H-pyrazol-5-yl]amino}-4-pyridinyl)amino]-N(methyloxy)benzamide
CBNumber: CB83044319
Molecular Formula: C20H23ClN6O2
Formula Weight: 414.89
MOL File: 1224887-10-8.mol

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GSK-2256098 Property

Density: 1.32±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO:47.33(Max Conc. mg/mL);114.08(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);72.31(Max Conc. mM)
Ethanol:56.0(Max Conc. mg/mL);134.98(Max Conc. mM)
Ethanol:PBS (pH 7.2) (1:4):0.2(Max Conc. mg/mL);0.48(Max Conc. mM)
form: A crystalline solid
pka: 5.24±0.10(Predicted)
color: White to khaki
InChI: InChI=1S/C20H23ClN6O2/c1-12(2)27-19(9-13(3)25-27)24-18-10-17(15(21)11-22-18)23-16-8-6-5-7-14(16)20(28)26-29-4/h5-12H,1-4H3,(H,26,28)(H2,22,23,24)
InChIKey: BVAHPPKGOOJSPU-UHFFFAOYSA-N
SMILES: C(NOC)(=O)C1=CC=CC=C1NC1C(Cl)=CN=C(NC2N(C(C)C)N=C(C)C=2)C=1

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H332Harmful if inhaled

H335May cause respiratory irritation

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P310Immediately call a POISON CENTER or doctor/physician.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 22955
Product name: GSK2256098
Purity: ≥98%
Packaging: 1mg
Price: $34
Updated: 2024/03/01

Cayman Chemical

Product number: 22955
Product name: GSK2256098
Purity: ≥98%
Packaging: 5mg
Price: $133
Updated: 2024/03/01

Cayman Chemical

Product number: 22955
Product name: GSK2256098
Purity: ≥98%
Packaging: 10mg
Price: $231
Updated: 2024/03/01

Cayman Chemical

Product number: 22955
Product name: GSK2256098
Purity: ≥98%
Packaging: 25mg
Price: $412
Updated: 2024/03/01

TRC

Product number: G797530
Product name: GSK2256098
Packaging: 2.5mg
Price: $145
Updated: 2021/12/16

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GSK-2256098 Chemical Properties,Usage,Production

Description

GSK2256098 is an inhibitor of focal adhesion kinase (FAK). It is selective for FAK, inhibiting only FAK greater than 50% in a panel of 261 kinases. GSK2256098 inhibits FAK autophosphorylation at tyrosine 397 (Y397) in OVCAR8 ovarian, U87MG glioblastoma, and A549 lung cancer cell lines (IC₅₀s = 15, 8.5, and 12 nM, respectively). It induces apoptosis and increases PARP levels, decreases viability (IC₅₀ = 25 μM), and inhibits colony formation in L3.6P1 cells. GSK2256098 (75 mg/kg per day) also leads to lower tumor weight and fewer metastases in the Ishikawa orthotopic mouse model of uterine cancer.

Uses

GSK 2256098 is FAK inhibitor. It can be used in biological study of molecular pathways: endothelial cell FAK-?A target for cancer treatment.

Synthesis

1201935-41-2

1124-16-9

1224887-10-8

Example 4: 1a Synthesis of 2-((5-chloro-2-((1-isopropyl-3-methyl-1H-pyrazol-5-yl)amino)pyridin-4-yl)amino)-N-methoxybenzamide 2-[(2,5-dichloro-4-pyridinyl)amino]-N-methoxybenzamide (70 mg, 0.224 mmol), 1-isopropyl-3-methyl-5-aminopyrazole (70 mg, 0.503 mmol) and cesium carbonate (230 mg, 0.706 mmol) were added sequentially to the microwave reaction tube. The reaction mixture was degassed with nitrogen for 10 min. BINAP (50 mg, 0.080 mmol) and palladium(II) acetate (10 mg, 0.045 mmol) were then added. The reaction mixture was placed in a microwave reactor and heated at 160 °C for 40 min. Upon completion of the reaction, the crude product was purified by reversed-phase high performance liquid chromatography (Gilson) using acetonitrile/water containing 0.1% formic acid as eluent to afford the target compound 2-((5-chloro-2-((1-isopropyl-3-methyl-1H-pyrazol-5-yl)amino)pyridin-4-yl)amino)-N-methoxybenzamide (15 mg, 15% yield). Mass spectrum (MS): M(C20H23ClN6O2)=414.89, (M+H)+=415,416; 1H NMR (400 MHz, chloroform-d) δ ppm 9.42(br.s, 1H), 8.71(br.s, 1H), 8.02(s, 1H), 7.54(br.s., 1H), 7.06(t, J= 7.5 Hz, 1H), 6.48(s, 1H), 6.32(br.s., 1H), 5.86(s, 1H), 4.47(dt, J=13.4,6.7 Hz, 1H), 3.92(s, 3H), 2.26(s, 3H), 1.41-1.43(d, J=6.6Hz, 6H).

in vivo

FAK is well-known to play an important role in angiogenesis, proliferation, and apoptosis, so the tumor samples harvested from the therapy experiments are examined. Evaluating CD31, significantly lower microvessel densities in tumors from mice treated with GSK2256098 and Paclitaxel is observed than in tumors from mice in the vehicle control group (P<0.05). This is consistent across both models, but Ishikawa tumors had the lowest microvessel density. All tumor models in mice treated with GSK2256098 exhibit less proliferation via Ki67 than control. Ishikawa tumors have the lowest Ki67 expression in response to therapy. Ishikawa tumors have higher apoptotic indices than Hec1A tumors after treatment with GSK2256098. Significant rates of apoptosis are seen in all models that had been treated with combination GSK2256098 and Paclitaxel^[2].

storage

Store at -20°C

References

[1] Patent: US2010/113475, 2010, A1. Location in patent: Page/Page column 23-24
[2] Patent: WO2013/3575, 2013, A1. Location in patent: Page/Page column 53

GSK-2256098 Preparation Products And Raw materials

Raw materials

Preparation Products

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GSK-2256098 Suppliers

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1224887-10-8, GSK-2256098Related Search:

GSK-3326595 GSK-2018682 GSK 2239633A GSK369796 MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel- GSK2636771 GSK-2881078 S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide 7Methyl-5-(1-{[3-(trifluoroMethyl)phenyl]acetyl}-2,3-dihydro1Hindol-5-yl)7Hpyrrolo[2,3d]pyriMidin-4-aMine GSK 2801 GSK2879552 GSK2795039 GSK 2330672 GSK2838232 GSK2126458 GSK-25 N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide GSK778

GSK-2256098

2-(5-chloro-2-(1-isopropyl-3-methyl-1H-pyrazol-5-ylamino)pyridin-4-ylamino)-N-methoxybenzamide

GTPL7939

Benzamide, 2-[[5-chloro-2-[[3-methyl-1-(1-methylethyl)-1H-pyrazol-5-yl]amino]-4-pyridinyl]amino]-N-methoxy-

2-[(5-chloro-2-{[3-methyl-1-(1-methylethyl)-1H-pyrazol-5-yl]amino}-4-pyridinyl)amino]-N(methyloxy)benzamide

CS-2424

FAK inhibitor GS2256098

GSK-2256098;GSK 2256098

GSK-2256099

GSK-2256098, GTPL7939

GSK2256098, 10 mM in DMSO

1224887-10-8

Inhibitors

APIs