N-[4-[(2-Amino-3-chloropyridin-4-yl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide

Product Name: N-[4-[(2-Amino-3-chloropyridin-4-yl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide
CAS No.: 1025720-94-8
Chemical Name: N-[4-[(2-Amino-3-chloropyridin-4-yl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide
Synonyms: CS-360;CS-1911;EOS-60544;ASLAN-002;BMS777607 (ASLAN-002);BMS 777607;BMS 817378;BMS 777607, 10 mM in DMSO;BMS777607; BMS-777607;BMS 777607;BMS-777607 BMS-817378 BMS777607 BMS817378;c-Met/HGFR,Inhibitor,Mer,inhibit,Axl,BMS817378,TAM Receptor,BMS 777607,Tyro3,BMS-817378
CBNumber: CB52589658
Molecular Formula: C25H19ClF2N4O4
Formula Weight: 512.89
MOL File: 1025720-94-8.mol

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N-[4-[(2-Amino-3-chloropyridin-4-yl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide Property

Boiling point:: 667.9±55.0 °C(Predicted)
Density: 1.49
storage temp.: Store at -20°C
solubility: ≥25.65 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
form: solid
pka: 10.54±0.70(Predicted)
color: White to off-white

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

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

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

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

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 18517
Product name: BMS-777607
Purity: ≥98%
Packaging: 1mg
Price: $37
Updated: 2024/03/01

Cayman Chemical

Product number: 18517
Product name: BMS-777607
Purity: ≥98%
Packaging: 5mg
Price: $142
Updated: 2024/03/01

Cayman Chemical

Product number: 18517
Product name: BMS-777607
Purity: ≥98%
Packaging: 10mg
Price: $249
Updated: 2024/03/01

Cayman Chemical

Product number: 18517
Product name: BMS-777607
Purity: ≥98%
Packaging: 50mg
Price: $793
Updated: 2024/03/01

TRC

Product number: A603310
Product name: N-[4-[(2-Amino-3-chloro-4-pyridinyl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-1,2-dihydro-2-oxo-3-pyridinecarboxamide
Packaging: 10mg
Price: $605
Updated: 2021/12/16

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N-[4-[(2-Amino-3-chloropyridin-4-yl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide Chemical Properties,Usage,Production

Uses

N-[4-[(2-amino-3-chloro-4-pyridinyl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-1,2-dihydro-2-oxo-3-pyridinecarboxamide is a selective and orally efficacious Inhibitor of the Met Kinase superfami ly.

Definition

ChEBI: N-[4-[(2-amino-3-chloro-4-pyridinyl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxo-3-pyridinecarboxamide is an aromatic amide.

Biological Activity

bms 777607 is a novel, selective and orally available atp-competitive met kinase inhibitor that primarily targets several met family members, including ron, met, tyro-3 and axi, with half maximal inhibitory concentration ic50 of 1.8 nmol/l, 3.9 nmol/l, 4.3 nmol/l and 1.1 nmol/l respectively. moreover, at higher concentrations, bms 777607 has been found to inhibit other protein tyrosine kinases, including mer, flt-3, aurora b, lck and vegfr2 with ic50 of 14 nmol/l, 16 nmol/l, 78 nmol/l, 120 nmol/l and 180 nmol/l respectively. in previous studies, bms 777607 potently inhibited the auto-phosphorylation of c-met (ic50: 20 nmol/l) leading to impaired xenograft growth.small-molecule inhibitor bms-777607 induces breast cancer cell polyploidy with increased resistance to cytotoxic chemotherapy agents. mol cancer ther. 2013 may;12(5):725-36. doi: 10.1158/1535-7163.mct-12-1079. epub 2013 mar 6.

Synthesis

1025721-14-5

1025720-94-8

3-Chloro-4-(4-(4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamido)-2-fluorophenoxy)pyridin-2-amine (1.2 g, 2.1 mmol) was used as a starting material and was dissolved in a solvent mixture of ethyl acetate (16 mL), acetonitrile (16 mL) and water (8 mL) at 0 °C. Subsequently, iodophenyl diacetate (820 mg, 2.6 mmol, Aldrich) was added. The reaction mixture was stirred at room temperature for 2 h before the crude product was collected by filtration. The solid was washed with additional ethyl acetate. The filtrate was washed with saturated aqueous sodium bicarbonate and the organic phase was dried with anhydrous sodium sulfate and subsequently concentrated under vacuum. The precipitate was combined with the concentrated filtrate and purified by rapid chromatography on silica gel (eluent: 2% methanol/chloroform) to afford the target compound, N-(4-((2-amino-3-chloropyridin-4-yl)oxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (810 mg, yield 74%). It was a white solid. The product was characterized by 1H NMR (DMSO-d6) and MS (ESI+): 1H NMR (DMSO-d6) δ 10.57 (s, 1H), 7.83-7.79 (m, 2H), 7.67 (d, 1H, J = 5.6Hz), 7.41-7.38 (m, 3H), 7.36-7.22 (m, 3H), 6.44 (d, 1H, J = 5.6Hz). 1H, J = 7.6 Hz), 6.36 (br s, 2H), 5.86 (d, 1H, J = 6.0 Hz), 4.18 (q, 2H, J = 7.2 Hz), 1.23 (t, 3H, J = 7.2 Hz); MS (ESI +) m/z 513.09 (M + H)+.

in vivo

Oral administration of BMS 777607 (6.25-50 mg/kg) significantly reduces tumor volumes of the GTL-16 human tumor xenografts in athymic mice with no observed toxicity^[1]. Administration of BMS 777607 (25 mg/kg/day) decreases the number of KHT lung tumor nodules (28.3%), improves the morphological hemorrhage, and significantly impairs the metastatic phenotype in the 6-8 week-old female C3H/HeJ mice injected with rodent fibrosarcoma KHT cells without apparent systemic toxicity compared to the control treatment. A low dose of BMS 777607 (10 mg/kg) also offers a mild but not significant inhibition of lung nodule formation compared to the vehicle control^[3].

IC 50

Axl; Tyro3

References

[1]dai y, siemann dw. bms-777607, a small-molecule met kinase inhibitor, suppresses hepatocyte growth factor-stimulated prostate cancer metastatic phenotype in vitro. mol cancer ther. 2010 jun;9(6):1554-61. doi: 10.1158/1535-7163.mct-10-0359. epub 2010 jun 1.
[2]sharma s, zeng jy, zhuang cm, zhou yq, yao hp, hu x, zhang r, wang mh.

N-[4-[(2-Amino-3-chloropyridin-4-yl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide Preparation Products And Raw materials

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N-[4-[(2-Amino-3-chloropyridin-4-yl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide Suppliers

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View Lastest Price from N-[4-[(2-Amino-3-chloropyridin-4-yl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide manufacturers

Dideu Industries Group Limited

Product: N-[4-[(2-Amino-3-chloropyridin-4-yl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide 1025720-94-8
Price: US $1.10/g
Min. Order: 1g
Purity: 99.00%
Supply Ability: 100 Tons min
Release date: 2021-09-07

1025720-94-8, N-[4-[(2-Amino-3-chloropyridin-4-yl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamideRelated Search:

2-Amino-4-chloropyridine Pentachloropyridine Gefitinib Cabozantinib MK-2206 2HCl Quizartinib (AC220) MG-132 Erlotinib hydrochloride

CS-1911

N-[4-[(2-amino-3-chloro-4-pyridinyl)oxy]-3-fluorophenyl]-4-ethoxyphenyl(4-fluorophenyl)-1,2-dihydro-2-oxo-3-pyridinecarboxamide

BMS777607; BMS-777607;BMS 777607

CS-360

N-[4-[(2-Amino-3-chloropyridin-4-yl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide

N-[4-[(2-amino-3-chloro-4-pyridinyl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-1,2-dihydro-2-oxo-3-pyridinecarboxamide

N-[4-[(2-Amino-3-chloropyridin-4-yl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide BMS 777607

BMS777607 (ASLAN-002)

ASLAN-002

N-(4-((2-Amino-3-chloropyridin-4-yl)oxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2

EOS-60544

BMS 777607;BMS 817378

3-Pyridinecarboxamide, N-[4-[(2-amino-3-chloro-4-pyridinyl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-1,2-dihydro-2-oxo-

N-[4-[(2-Amino-3-chloropyridin-4-yl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide ISO 9001：2015 REACH

BMS-777607 BMS-817378 BMS777607 BMS817378

c-Met/HGFR,Inhibitor,Mer,inhibit,Axl,BMS817378,TAM Receptor,BMS 777607,Tyro3,BMS-817378

BMS 777607, 10 mM in DMSO

1025720-94-8

C25H19ClF2N4O4

Inhibitors