ChemicalBook > CAS DataBase List > FGF-401

FGF-401

Product Name
FGF-401
CAS No.
1708971-55-4
Chemical Name
FGF-401
Synonyms
Roblitinib;0997;FGF-401;NVP-FGF-401;EVER-4010001;FGF 401;FGF-401;FGF401( Roblitinib);Roblitinib（FGF-401）;FGF-401 (NVP-FGF401;Roblitinib, 10 mM in DMSO
CBNumber
CB03166185
Molecular Formula
C25H30N8O4
Formula Weight
506.56
MOL File
1708971-55-4.mol
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FGF-401 Property

Boiling point:
852.1±65.0 °C(Predicted)
Density 
1.39±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:5.4(Max Conc. mg/mL);10.66(Max Conc. mM)
Chloroform:30.0(Max Conc. mg/mL);59.22(Max Conc. mM)
form 
A crystalline solid
pka
11.40±0.20(Predicted)
color 
White to off-white
InChIKey
BHKDKKZMPODMIQ-UHFFFAOYSA-N
SMILES
N1(C(NC2=NC=C(C#N)C(NCCOC)=C2)=O)C2C(=CC(CN3CCN(C)CC3=O)=C(C=O)N=2)CCC1
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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
23029
Product name
FGF401
Packaging
1mg
Price
$38
Updated
2024/03/01
Cayman Chemical
Product number
23029
Product name
FGF401
Packaging
5mg
Price
$166
Updated
2024/03/01
Cayman Chemical
Product number
23029
Product name
FGF401
Packaging
10mg
Price
$292
Updated
2024/03/01
Cayman Chemical
Product number
23029
Product name
FGF401
Packaging
25mg
Price
$638
Updated
2024/03/01
ChemScene
Product number
CS-6853
Product name
Roblitinib
Purity
99.33%
Packaging
50mg
Price
$690
Updated
2021/12/16
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FGF-401 Chemical Properties,Usage,Production

Description

FGF401 is an inhibitor of FGF receptor 4 (FGFR4; IC50 = 1.9 nM). It inhibits proliferation of Huh7 carcinoma cells with an IC50 value of 12 nM. FGF401 induces bile acid synthesis in dogs, increasing plasma and fecal levels of bile acids when administered at a dose of 45 mg/kg per day for four weeks. It also decreases serum cholesterol when administered at doses ranging from 5 to 45 mg/kg per day.

Uses

Roblitinib (FGF-401) is an orally active and highly selective FGFR4 inhibitor with an IC50 of 1.9 nM[1]. Roblitinib has antitumor activity[2].

in vivo

Roblitinib (gavage; 10-100 mg/kg; b.i.d.; for 10 days) with the 30 mg/kg has the maximal level of inhibition of FGFR4-dependent tumor growth in the Hep3B xenograft model[1].
Roblitinib causes blood concentrations dropped below the IC90 threshold level within 8 h of dosing, and controlles tumor growth to the level of stasis at the lowest dose of 10 mg/kg for 6 days[1].
Roblitinib (iv at 1 mg/kg; po at 3 mg/kg) has a T1/2 of 1.4 hours, a CL of 28 mL/min kg, and a Vss of 2.3 L/kg for Male mice (C57BL/6) [1].
Roblitinib (iv at 0.5 mg/kg; po at 3 mg/kg) has a T1/2 of 4.4 hours, a CL of 19 mL/min kg, and a Vss of 3.9 L/kg for male SD rats[1].

Animal Model:Male Wistar Hannover rats (Hep3B xenograft model)[1]
Dosage:10, 30, 100 mg/kg
Administration:Gavage; for 10 days
Result:Caused blood concentrations dropped below the IC90 threshold between 8 and 12 h following dosing.
Had the maximal level of inhibition of FGFR4-dependent tumor growth in the Hep3B xenograft model.
Animal Model:Male mice (C57BL/6)[1]
Dosage:1 mg/kg or 3 mg/kg (Pharmacokinetic Analysis)
Administration:IV at 1 mg/kg; PO at 3 mg/kg
Result:Had a T1/2 of 1.4 hours, a CL of 28 mL/min?kg, and a Vss of 2.3 L/kg.

IC 50

FGFR4: 1.9 nM (IC50); FGFR1: >10 μM (IC50); FGFR2: >10 μM (IC50); FGFR3: >10 μM (IC50); rat FGFR4: >10 μM (IC50)

References

[1] Nicole Buschmann, et al. Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors. WO2015059668A1.
[2] Robin A Fairhurst, et al. Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. J Med Chem. 2020 Nov 12;63(21):12542-12573. DOI:10.1021/acs.jmedchem.0c01019

FGF-401 Preparation Products And Raw materials

Raw materials

Preparation Products

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FGF-401 Suppliers

China 115 United States 6 USA 1 Global 122
Shanghai Synchem Pharma Co., ltd
Tel
21-619849051-1 18521059765
Email
synchempharma@aliyun.com
Country
China
ProdList
6468
Advantage
55
Shanghai Dongyang Biotechnology Co., Ltd.
Tel
0512-0512-13601744364 13601744364
Email
chemsharker@126.com
Country
China
ProdList
1010
Advantage
58
Kaixin Chemical (Hong Kong) Limited
Tel
010-88886666-01 13112345678
Fax
CDXH21@126.com
Email
loyson@tcypharm.com
Country
China
ProdList
597
Advantage
55
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Jia Xing Isenchem Co.,Ltd
Tel
0573-85285100 18627885956
Fax
0573-85285100
Email
isenchem@163.com
Country
China
ProdList
9310
Advantage
66
Shanghai Feibo Chemical Technology Co., Ltd
Tel
021-58955608,2250286 15921236618
Email
blinkzeng@gmail.com
Country
China
ProdList
522
Advantage
62
Guangzhou Isun Pharmaceutical Co., Ltd
Tel
020-39119399 18927568969
Fax
020-39119999
Email
isunpharm@qq.com
Country
China
ProdList
4720
Advantage
55
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3506
Advantage
58
Changzhou Renaissance Chem Co. Ltd
Tel
86-519-86202821
Fax
Email： sales@rosewellchem.com
Country
China
ProdList
116
Advantage
56
ChemStrong Scientific Co.,Ltd
Tel
0755-0755-66853366 13670046396
Fax
0755-28363542
Email
sales@chem-strong.com
Country
China
ProdList
18333
Advantage
56
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View Lastest Price from FGF-401 manufacturers

Career Henan Chemical Co
Product
8-naphthyridine-1(2H)-carboxamide 1708971-55-4
Price
US $9.80/KG
Min. Order
1g
Purity
≥99%
Supply Ability
100kg
Release date
2019-12-25

1708971-55-4, FGF-401Related Search:

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  • N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide
  • N-[5-cyano-4-(2-methoxyethylamino)pyridin-2-yl]-7-formyl-6-[(4-methyl-2-oxopiperazin-1-yl)methyl]-3,4-dihydro-2~{H}-1,8-naphthyridine-1-carboxamide
  • Roblitinib（FGF-401）
  • FGF 401;FGF-401
  • 8-naphthyridine-1(2H)-carboxamide
  • 0997
  • N-[5-Cyano-4-[(2-methoxyethyl)amino]-2-pyridinyl]-7-formyl-3,4-dihydro-6-[(4-methyl-2-oxo-1-piperazinyl)methyl]-1,8-naphthyridine-1(2H)-carboxamide
  • Roblitinib
  • 1,8-Naphthyridine-1(2H)-carboxamide, N-[5-cyano-4-(2-methoxyethyl)amino]-2-pyridinyl]-7-formyl-3,4-dihydro-6-[(4-methyl-2-oxo-1-piperazinyl)methyl]-
  • FGF-401
  • FGF401( Roblitinib)
  • FGF-401 ISO 9001：2015 REACH
  • N-{5-cyano-4-[(2-methoxyethyl)amino]pyridin-2-yl}-7-formyl-6-[(4-methyl-2-oxopiperazin-1-yl)methyl]-1,2,3,4-tetrahydro-1,8-naphthyridine-1-carboxamide
  • Roblitinib, 10 mM in DMSO
  • EVER-4010001
  • NVP-FGF-401
  • Roblitinib (FGF401) ，S8548
  • FGF-401 (NVP-FGF401
  • 1708971-55-4
  • API