Binding Mode
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BIBF-1120

Binding Mode
Product Name
BIBF-1120
CAS No.
928326-83-4
Chemical Name
BIBF-1120
Synonyms
CS-76;BIBF-1120;Nintedanib;Trinidad Neeb;VargatefTM BIBF;Nintedanib, >=98%;BIBF-1120(Vargatef);BIBF1120 nintedanib;Intedanib(BIBF-1120);928326-83-4 BIBF-1120
CBNumber
CB92467147
Molecular Formula
C31H33N5O4
Formula Weight
539.633
MOL File
928326-83-4.mol
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

American Custom Chemicals Corporation
Product number
KIN0000342
Product name
BIBF-1120
Purity
95.00%
Packaging
5MG
Price
$480
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
KIN0000342
Product name
BIBF-1120
Purity
95.00%
Packaging
5G
Price
$6121.5
Updated
2021/12/16
A1 Biochem Labs
Product number
A1-04307
Product name
Nintedanib Esylate(BIBF-1120)
Packaging
2.5g
Price
$1300
Updated
2021/12/16
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BIBF-1120 Chemical Properties,Usage,Production

Binding Mode

In the co-crystal structure of nintedanib in complex with VEGFR2, the indolinone core binds to the hinge, forming two hydrogen bonds: the NH group of the indolinone with the amide oxygen of Glu917, and the carbonyl oxygen of the indolinone with the amide NH of Cys919. The methyl ester carbonyl oxygen hydrogen bonds with the side chain amine of Lys868. The external solvent exposed N-methyl amine of piperazine potentially engages in ionic interactions with the carboxylic acid reside of Glu850. An X-ray co-crystal structure of RET kinase domain–nintedanib complex has also been determined. It binds to the RET kinase via three crucial hydrogen bond interactions similar to those observed in its complex with VEGFR2.

Description

BIBF 1120 is a triple kinase inhibitor blocking vascular endothelial growth factor receptor, PDGF receptor, and FGF receptor, which has a potential to inhibit tumor growth and pulmonary fibrosis.

Characteristics

Primary targets: PDGFR; VEGFR; FGFR
Class: receptor tyrosine kinase
Treatment: ILD, IPF
Oral bioavailability = 4.7%
Elimination half-life = 10

Definition

ChEBI: Nintedanib is a member of the class of oxindoles that is a kinase inhibitor used (in the form of its ethylsulfonate salt) for the treatment of idiopathic pulmonary fibrosis and cancer. It has a role as an antineoplastic agent, a tyrosine kinase inhibitor, a vascular endothelial growth factor receptor antagonist, a fibroblast growth factor receptor antagonist and an angiogenesis inhibitor. It is an aromatic ester, a methyl ester, a member of oxindoles, an enamine, an aromatic amine, an aromatic amide and a N-alkylpiperazine. It is a conjugate base of a nintedanib(1+).

brand name

OfevTM

Anticancer Research

BIBF 1120 is a potent inhibitor of VEGFR as well as PDGF and fibroblast growth factor receptor. In a randomized phase II placebo-controlled trial, patients who had just completed chemotherapy for relapsed ovarian cancer, with evidence of response, but at high risk of further early recurrence were treated with BIBF 1120. The study drug was taken continuously (28-day cycles) for 9 cycles (36 weeks) or until disease progression or patient withdrawal. The 36-week PFS 26-week rates were 16.3% and 5.0% in the BIBF 1120 and placebo groups, respectively (HR 0.65; 95% Cl, 0.42 to 1.02; P = .06). Toxicity was also well tolerated.This has prompted a phase III trial (NCTO1O15118) where BIBF 1120 will be combined with carboplatin/paclitaxel as front-line chemotherapy in ovarian cancer.

Side effects

Most of the adverse effects associated with BTBF-1120 were tolerable. They include diarrhea, nausea, vomiting, abdominal pain, and reversible increase in liver enzymes.

Clinical claims and research

BIBF 1120 is a triple tyrosine kinase inhibitor with efficacy on fibroblast growth factor (FGF), vascular endothelial growth factor (VEGF), and on platelet-derived growth factor (PDGF).The activation of these pathways has been implicated in the pathogenesis of experimental fibrosis. In a 12-month phase II trial (the TOMORROW trial) patients who received 150 mg of BIBF 1120 twice daily had a trend toward reduction in the decline of FVC.In addition, there was an improved QOL and a reduction in acute exacerbations of IPF. These results led to a phase III trial. This was designed as two identical phase III studies called INPULSIS-1 and INPULSIS-2. The INPULSIS trials tested the effect on IPF disease progression over 52 weeks using 150 mg of twice daily nintedanib (formerly BIBF 1200) versus placebo. The inclusion criteria included patients diagnosed with idiopathic pulmonary fibrosis based on established criteria.In addition, the participants’ HRCT scans and biopsies, if available, were reviewed by a central radiologist or pathologist to confirm the diagnosis. Enrolled subjects had a FVC which was >50% of the predicted value and a DlCO from 30–79% of predicted values. Published data from the two trials indicated that patients who received nintedanib demonstrated a statistically significant reduction in the rate of decline in lung function compared with the placebo group. In the INPULSIS-2 trial, there was a significant reduction in the time to first acute exacerbation of IPF. This was not replicated in the INPULSIS-1 trial data. The most common side effect for the medication was diarrhea. On the basis of this study, nintedanib is pending evaluation for approval for use in the United States.

BIBF-1120 Preparation Products And Raw materials

Raw materials

Preparation Products

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BIBF-1120 Suppliers

Sequoia Research Products Ltd.
Tel
--
Fax
--
Email
sales@seqchem.com
Country
United Kingdom
ProdList
3113
Advantage
69
Sinbond Industiral Co., Ltd.
Tel
--
Fax
--
Email
cici1124@gmail.com
Country
United Kingdom
ProdList
248
Advantage
50
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View Lastest Price from BIBF-1120 manufacturers

Shaanxi TNJONE Pharmaceutical Co., Ltd
Product
Bibf 1120; Nintedanib 928326-83-4
Price
US $0.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
10000kg
Release date
2024-05-13
Zhuozhou Wenxi import and Export Co., Ltd
Product
Nintedanib (BIBF 1120) 928326-83-4
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-10
Zhuozhou Wenxi import and Export Co., Ltd
Product
Nintedanib (BIBF 1120) 928326-83-4
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-09