Brivanib - CAS 649735-46-6
Catalog number:
649735-46-6
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
Inquire
Targets:
VEGFR
Description:
Brivanib is the hydrolyzed form of Brivanib alaninate, which is a vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with potential antineoplastic activity. Brivanib strongly binds to and inhibits VEGFR2, a tyrosine kinase receptor expressed almost exclusively on vascular endothelial cells; inhibition of VEGFR2 may result in inhibition of tumor angiogenesis, inhibition of tumor cell growth, and tumor regression. Check for active clinical trials or closed clinical trials using this agent.
Publictions citing BOC Sciences Products
  • >> More
Synonyms:
BMS-540215
MSDS:
Inquire
Current Developer:
Bristol-Myers Squibb.
1.Evaluating the role of treatment-related toxicities in the challenges facing targeted therapies for advanced hepatocellular carcinoma.
Palmer DH1, Johnson PJ2. Cancer Metastasis Rev. 2015 Sep;34(3):497-509. doi: 10.1007/s10555-015-9580-2.
Advanced hepatocellular carcinoma (aHCC) is a complex disease beset by underlying liver dysfunction and high molecular heterogeneity. Sorafenib, introduced in 2007, is considered the standard systemic therapy for aHCC, yet only a minority of patients show objective evidence of a response radiologically, and median overall survival is still under 1 year. Other targeted drugs for the treatment of aHCC have failed to reach their primary endpoints of improved/non-inferior overall survival in comparison with sorafenib in recent phase 3 trials. Toxicity was a significant problem, raising the question as to whether outcomes in aHCC trials are being hindered by high levels of adverse events (AEs), particularly in populations with underlying cirrhosis. This is true of six recently failed phase 3 studies involving sunitinib, erlotinib, linifanib, brivanib (two trials), and everolimus, as well as ongoing phase 2 and 3 trials of other drugs that work through similar molecular pathways.
2.Targeting angiogenesis in endometrial cancer - new agents for tailored treatments.
Papa A1, Zaccarelli E1, Caruso D1, Vici P2, Benedetti Panici P3, Tomao F3. Expert Opin Investig Drugs. 2016 Jan;25(1):31-49. doi: 10.1517/13543784.2016.1116517. Epub 2015 Dec 19.
INTRODUCTION: Endometrial carcinoma represents the most frequent gynecologic tumor in developed countries. The majority of women presents with low-grade tumors but a significant subset of women experience recurrence and do not survive their disease. Patients with stage III/ IV or recurrent endometrial cancer have a poor prognosis. Identification of active and tolerable new targeted agents versus specific molecular targets is a priority objective. Angiogenesis is a complex process that plays a crucial role in the development of many types of cancer and in particular endometrial cancer.
3.Effect of milling temperatures on surface area, surface energy and cohesion of pharmaceutical powders.
Shah UV1, Wang Z1, Olusanmi D2, Narang AS2, Hussain MA2, Tobyn MJ3, Heng JY4. Int J Pharm. 2015 Nov 10;495(1):234-40. doi: 10.1016/j.ijpharm.2015.08.061. Epub 2015 Aug 24.
Particle bulk and surface properties are influenced by the powder processing routes. This study demonstrates the effect of milling temperatures on the particle surface properties, particularly surface energy and surface area, and ultimately on powder cohesion. An active pharmaceutical ingredient (API) of industrial relevance (brivanib alaninate, BA) was used to demonstrate the effect of two different, but most commonly used milling temperatures (cryogenic vs. ambient). The surface energy of powders milled at both cryogenic and room temperatures increased with increasing milling cycles. The increase in surface energy could be related to the generation of surface amorphous regions. Cohesion for both cryogenic and room temperature milled powders was measured and found to increase with increasing milling cycles. For cryogenic milling, BA had a surface area ∼ 5× higher than the one obtained at room temperature. This was due to the brittle nature of this compound at cryogenic temperature.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related VEGFR Products


CAS 417716-92-8 Lenvatinib

Lenvatinib
(CAS: 417716-92-8)

Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more s...

CAS 1308672-74-3 Sulfatinib

Sulfatinib
(CAS: 1308672-74-3)

Sulfatinib, an oral drug candidate, is a small molecule inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3, and the fibroblast growth...

CAS 1218779-75-9 Apatinib

Apatinib
(CAS: 1218779-75-9)

Apatinib mesylate is an orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. Apa...

CAS 649735-46-6 Brivanib

Brivanib
(CAS: 649735-46-6)

Brivanib is the hydrolyzed form of Brivanib alaninate, which is a vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with potential antineoplastic...

CAS 755037-03-7 Regorafenib

Regorafenib
(CAS: 755037-03-7)

Regorafenib, also known as BAY 73-4506, is an orally bioavailable small molecule with potential antiangiogenic and antineoplastic activities. Regorafenib binds ...

CAS 168835-82-3 SU1498

SU1498
(CAS: 168835-82-3)

SU1498 is a selective inhibitor of the receptor tyrosine kinase VEGF receptor 2 (VEGFR2, aka FLK1; IC50 = 700 nM), and inhibits Flk-1 with an IC50 of value of 7...

CAS 193000-39-4 ZM323881 hydrochloride

ZM323881 hydrochloride
(CAS: 193000-39-4)

Potent and selective inhibitor of VEGFR2 (IC50: 2 nM for VEGFR2 vs >50 mM for VEGFR1 respectively)

CAS 1433953-83-3 SAR131675

SAR131675
(CAS: 1433953-83-3)

SAR131675 dose dependently inhibits the proliferation of primary human lymphatic cells, induced by the VEGFR-3 ligands VEGFC and VEGFD, with an IC50 of about 20...

CAS 10537-47-0 Tyrphostin 9

Tyrphostin 9
(CAS: 10537-47-0)

Tyrphostin 9 is firstly designed as an EGFR inhibitor with IC50 of 460 μM, but is also found to be more potent to PDGFR with IC50 of 0.5 μM.

ARQ 736 disodium salt
(CAS: 1228237-57-7)

This active molecular is a Proto oncogene protein b raf and Vascular endothelial growth factor A inhibitor originated by ArQule. ARQ 736 is effective in killing...

BRN-103
(CAS: 1346265-80-2)

BRN-103 can suppress the phosphorylation of vascular endothelial growth factor (VEGF) receptor 2. It can also inhibit the activations of AKT and eNOS. These res...

TAS-115
(CAS: 1190836-34-0)

This active molecular is a c-MET and VEGFR inhibitor which is selective and specific in vitro. In vivo studies, TAS-115 suppressed the progression of MET-inacti...

CAS 1019206-88-2 Regorafenib monohydrate

Regorafenib monohydrate
(CAS: 1019206-88-2)

Regorafenib monohydrate is a multitargetedinhibitor of tyrosine kinase with IC50 values of 13nM, 4.2nM, 46nM, 2.5nM, 28nM, 19nM, 202nM, 22nM, 7nM, 1.5nM and 311...

CAS 857036-77-2 Cediranib maleate

Cediranib maleate
(CAS: 857036-77-2)

Cediranib maleate is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM. It also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM. It inhibits VEGF-stimulated proli...

CAS 228559-41-9 Ki8751

Ki8751
(CAS: 228559-41-9)

Ki8751 is a potent, selective inhibitor of VEGFR-2 tyrosine kinase (IC50 = 0.9 nM). Displays some inhibitory activity towards c-Kit, PDGFRα and FGFR-2 (IC50 val...

CAS 408502-06-7 KDR-in-4

KDR-in-4
(CAS: 408502-06-7)

A potent kinase insert domain-containing receptor (KDR/VEGFR2) inhibitor (IC50= 7 nM)

CAS 338992-53-3 Vandetanib trifluoroacetate

Vandetanib trifluoroacetate
(CAS: 338992-53-3)

Vandetanib is an anti-cancer drug that is used for the treatment of certain tumours of thethyroid gland. It acts as a kinase inhibitor of a number of cell recep...

CAS 835621-07-3 Regorafenib Hydrochloride

Regorafenib Hydrochloride
(CAS: 835621-07-3)

Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1.

CAS 300842-64-2 NVP-ACC789

NVP-ACC789
(CAS: 300842-64-2)

NVP-ACC789 is a potent, selective and orally active inhibitor of the VEGF receptor tyrosine kinases, antagonizing tumor-driven angiogenesis

CAS 1018069-81-2 TG 100801 Hydrochloride

TG 100801 Hydrochloride
(CAS: 1018069-81-2)

TG 100801 is the prodrug of TG 100572, which is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kin...

Chemical Structure

CAS 649735-46-6 Brivanib

Quick Inquiry

Verification code

Featured Items