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Brivanib

Product Name
Brivanib
CAS No.
649735-46-6
Chemical Name
Brivanib
Synonyms
CS-75;Brivanib;Bms540215;Bms 540215;Unii-ddu33B674i;Brivanib, >=98%;Brivanib(BMS-540215);BMS540215; BMS 540215;Brivanib, 10 mM in DMSO;Tyrosine Kinase Inhibitor
CBNumber
CB92484687
Molecular Formula
C19H19FN4O3
Formula Weight
370.38
MOL File
649735-46-6.mol
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Brivanib Property

Density 
1.42
storage temp. 
Store at -20°C
solubility 
insoluble in H2O; ≥18.5 mg/mL in DMSO; ≥3.39 mg/mL in EtOH with ultrasonic
form 
Yellow powder.
pka
14.18±0.20(Predicted)
color 
White to light brown
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H360May damage fertility or the unborn child

H361Suspected of damaging fertility or the unborn child

H373May cause damage to organs through prolonged or repeated exposure

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P281Use personal protective equipment as required.

P308+P313IF exposed or concerned: Get medical advice/attention.

P314Get medical advice/attention if you feel unwell.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML3671
Product name
Brivanib
Purity
≥98% (HPLC)
Packaging
5MG
Price
$116.85
Updated
2025/07/31
Sigma-Aldrich
Product number
SML3671
Product name
Brivanib
Purity
≥98% (HPLC)
Packaging
25MG
Price
$494
Updated
2025/07/31
Cayman Chemical
Product number
23690
Product name
Brivanib
Purity
≥95%
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
23690
Product name
Brivanib
Purity
≥95%
Packaging
5mg
Price
$131
Updated
2024/03/01
Cayman Chemical
Product number
23690
Product name
Brivanib
Purity
≥95%
Packaging
10mg
Price
$214
Updated
2024/03/01
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Brivanib Chemical Properties,Usage,Production

Uses

Brivanib is an ATP-competitive inhibitor against human VEGFR2 and FGFR with IC50 of 25 nM and 148 nM, respectively.

Definition

ChEBI: Brivanib is a secondary alcohol resulting from the hydrolysis of the carboxylic ester group of brivanib alaninate. It is a dual VEGFR-2/FGFR-1 kinase inhibitor whose alanine prodrug, brivanib alaninate is currently under development as an oral agent for the treatment of cancer. It has a role as an antineoplastic agent, an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, an angiogenesis inhibitor, an apoptosis inducer, a fibroblast growth factor receptor antagonist and a drug metabolite. It is a pyrrolotriazine, a fluoroindole, a diether, an aromatic ether and a secondary alcohol.

Biological Activity

brivanib is an atp competitive inhibitor of human vegfr-2 with ic50 value of 25nm [1].brivanib is a selective rtk inhibitor that targets signaling via vegfr2 and 3, and fgfr1, 2 and 3. targeting both vegf and fgf signaling pathways inhibits tumor growth in rt2 mice, with vegf signaling predominating in initiation of tumor angiogenesis, currently, brivanib therapy is being evaluated in phase iii

in vivo

Brivanib displays antitumor activities in H3396 xenograft in athymic mice. At a dose of 60 and 90 mg/kg (p.o.), brivanib completely inhibits the tumor growth, with TGI of 85% and 97%, respectively[1]. Moreover, brivanib significantly suppresses tumor growth in Hepatocellular carcinoma (HCC) xenografts, which due to the decrease in phosphorylation of VEGFR2. The results show that the tumor weights in 06-0606 xenograft mice are 55% and 13%, compared with the controls at a dose of 50 mg/kg and 100 mg/kg. Brivanib is suggested to be efficient in treatment of HCC[2]. Brivanib (50 mg/kg, p.o.) attenuates liver fibrosis and stellate cell activation induced by BDL in mice. Brivanib inhibits growth factor and growth factor receptor mRNA expression in sham control animals but shows variable effects in bile duct ligated animals[3].

target

VEGFR-2

IC 50

VEGFR2: 25 nM (IC50)

References

[1] rajeev s. bhide, zhen-wei cai, yong-zheng zhang, ligang qian, donna wei, stephanie barbosa, louis j. lombardo, robert m. borzilleri, xiaoping zheng, laurence i. wu, joel c. barrish, soong-hoon kim, kenneth leavitt, arvind mathur, leslie leith, sam chao, barri wautlet, steven mortillo, robert jeyaseelan sr., daniel kukral, john t. hunt, amrita kamath, aberra fura, viral vyas, punit marathe, celia d’arienzo, george derbin, and joseph fargnoli. discovery and preclinical studies of (r)-1-(4-(4-fluoro-2-methyl-1h-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-ol (bms-540215), an in vivo active potent vegfr-2 inhibitor. journal of medicinal chemistry. 2006, 49 (7): 2143-2146.
[2] elizabeth allen, ian b. walters, and douglas hanahan. brivanib, a dual fgf/vegf inhibitor, is active both first and second line against mouse pancreatic neuroendocrine tumors developing adaptive/evasive resistance to vegf inhibition. clinical cancer research. 2011 (17): 5299-5310.

Brivanib Preparation Products And Raw materials

Raw materials

Preparation Products

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Brivanib Suppliers

AdooQ BioScience, LLC
Tel
+1 (866) 930-6790
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+1 (866) 333-9607
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info@adooq.com
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United States
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Target molecule Corp.
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857-239-0968
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857-239-8801
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service1@targetmol.com
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United States
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2559
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60
Musechem
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+1-800-259-7612
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+1-800-259-7612
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info@musechem.com
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United States
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InvivoChem
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+1-708-310-1919 +1-13798911105
Fax
708-557-7486
Email
sales@invivochem.cn
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United States
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Cckinase, Inc.
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+1 (732)236-3202
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sales@cckinase.com
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United States
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BOC Sciences
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+1-631-485-4226
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1-631-614-7828
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inquiry@bocsci.com
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United States
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Alchem Pharmtech,Inc.
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8485655694
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sales@alchempharmtech.com
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United States
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Aladdin Scientific
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TargetMol Chemicals Inc.
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+1-781-999-5354;
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support@targetmol.com
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Aceschem Inc.
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+1-817863-6948 +1-(817)863-6948
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sales@aceschem.com
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ApexBio Technology
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Cayman Chemical Company
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Creative Enzymes
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Matrix Scientific
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Selleck Chemicals LLC
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Santa Cruz Biotechnology, Inc.
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Exlcusive Chemistry Ltd
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AK Scientific, Inc.
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View Lastest Price from Brivanib manufacturers

Career Henan Chemical Co
Product
1-[[4-[(4-Fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxy]-2-propanol 649735-46-6
Price
US $2.00/KG
Min. Order
1g
Purity
98%min
Supply Ability
ask
Release date
2020-01-08

649735-46-6, BrivanibRelated Search:


  • 1-[[4-[(4-Fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxy]-2-propanol
  • (R)-1-(4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo(2,1-F)(1,2,4)triazin-6-yloxy)propan-2-ol
  • 2-Propanol, 1-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-5-methylpyrrolo(2,1-F)(1,2,4)triazin-6-yl)oxy)-, (2R)-
  • Bms 540215
  • Bms540215
  • Unii-ddu33B674i
  • 1-[4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-5-methyl-pyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-propan-2(R)-ol
  • (R)-1-(4-(4-Fluoro-2-Methyl-1H-indol-5-yloxy)-5-Methylpyrrolo[1,2-f][1,2,4]triazin-6-yloxy)propan-2-ol
  • Brivanib(BMS-540215)
  • Brivanib
  • Tyrosine Kinase Inhibitor
  • (R)-1-(4-(4-fluoro-2-Methyl-1H-indol-5-yloxy)-5-Methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-ol, BSM-540215
  • (2R)-1-[4-(4-Fluoro-2-Methyl-1H-indol-5-yloxy)-5-Methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]propanol
  • (2R)-1-({4-[(4-fluoro-2-Methyl-1H-indol-5-yl)oxy]-5-Methylpyrrolo[2,1-f][1,2,4]triazin-6-yl}oxy)propan-2-ol
  • (2R)-1-[4-[(4-Fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methyl-pyrrolo[2,1-f][1,2,4]triazin-6-yl]oxypr
  • Brivanib, >=98%
  • (2R)-1-[4-[(4-Fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methyl-pyrrolo[2,1-f][1,2,4]triazin-6-yl]ox
  • 1-[[4-[(4-Fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo-[2,1-f][1,2,4]triazin-6-yl]oxy]-2
  • CS-75
  • BMS540215; BMS 540215
  • 1-[[4-[(4-Fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxy]-2-propanol USP/EP/BP
  • (2R)-1-({4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpy...
  • Brivanib/Tyrosine Kinase Inhibitor
  • Brivanib, 10 mM in DMSO
  • 649735-46-6
  • Inhibitors