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Orantinib (SU6668)

Product Name
Orantinib (SU6668)
CAS No.
252916-29-3
Chemical Name
Orantinib (SU6668)
Synonyms
TSU-68;Orantinib;NSC 702827;TSU-68, >=99%;Orantinib (SU;TSU-68 (SU6668);SU 6668(TSU-68);Orantinib (SU6668;Orantinib (TSU-68);TSU-68 (Orantinib,SU6668)
CBNumber
CB31456201
Molecular Formula
C18H18N2O3
Formula Weight
310.35
MOL File
252916-29-3.mol
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Orantinib (SU6668) Property

Melting point:
252-254 °C
Boiling point:
590.5±50.0 °C(Predicted)
Density 
1.328±0.06 g/cm3(Predicted)
storage temp. 
Store at RT
solubility 
DMSO (Slightly), Methanol (Slightly)
form 
Solid
pka
4?+-.0.10(Predicted)
color 
Orange to Brown
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H301Toxic if swalloed

H318Causes serious eye damage

H361Suspected of damaging fertility or the unborn child

H372Causes 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.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

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

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

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

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

P314Get medical advice/attention if you feel unwell.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
13873
Product name
SU 6668
Purity
≥98%
Packaging
1mg
Price
$31
Updated
2024/03/01
Cayman Chemical
Product number
13873
Product name
SU 6668
Purity
≥98%
Packaging
5mg
Price
$73
Updated
2024/03/01
Cayman Chemical
Product number
13873
Product name
SU 6668
Purity
≥98%
Packaging
10mg
Price
$121
Updated
2024/03/01
Usbiological
Product number
022488
Product name
TSU-68
Packaging
10mg
Price
$396
Updated
2021/12/16
TRC
Product number
T797550
Product name
TSU-68
Packaging
50mg
Price
$425
Updated
2021/12/16
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Orantinib (SU6668) Chemical Properties,Usage,Production

Uses

TSU-68 is a inhibitor that targets vascular endothelial growth factor receptor 2, platelet-derived growth factor receptor β, and fibroblast growth factor receptor 1. The inhibitory effects of TSU-68 towards these growth factors lead to substantial antitumor activity and showed potential in its development in therapeutic uses.

Uses

3-[2,4-dimethyl-5-[(E)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid is a potent inhibitor of Flk-1/KDR, FGFR1 and PDGFRβ with Ki of 2.1 μM, 1.2 μM, and 8 nM, respectively.

Definition

3-[2,4-dimethyl-5-[(E)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid is an oxindole that is 3-methyleneoxindole in which one of the hydrogens of the methylene group is substituted by a 2-(2-carboxyethyl)-3,5-dimethylpyrrol-3-yl group. It is an ATP-competitive inhibitor of the tyrosine kinase activity of fibroblast growth facto receptor 1.

Biological Activity

ATP-competitive PDGFR, VEGF and FGFR inhibitor (IC 50 values are 0.06, 2.43, 3.04 and > 100 μ M at PDGFR β , VEGFR2, FGFR1 and EGFR respectively). Inhibits proliferation of HUVEC and NIH3T3 cells in vitro (IC 50 values are 0.41, 9.3 and 16.5 μ M for VEGF, FGF and PDGF-stimulated growth respectively) and induces > 75% growth inhibition against a broad range of tumor types in vivo . Exhibits antiangiogenic, anti-inflammatory, antimetastatic and proapoptotic activity and is orally active.

in vitro

biochemical kinetic studies using isolated flk-1, fgf receptor 1, and pdgf receptor β kinases revealed that tsu-68 has competitive inhibitory properties with respect to atp. in cellular systems, tsu-68 inhibited receptor tyrosine phosphorylation and mitogenesis after stimulation of cells by appropriate ligands [1].

in vivo

oral or i.p. administration of tsu-68 in athymic mice resulted in significant growth inhibition of a diverse panel of human tumor xenografts of glioma, melanoma, lung, colon, ovarian, and epidermoid origin [1].

storage

Store at RT

References

[1] laird ad, vajkoczy p, shawver lk et al. su6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors. cancer res. 2000 aug 1;60(15):4152-60.
[2] okamoto i, yoshioka h, takeda k et al. phase i clinical study of the angiogenesis inhibitor tsu-68 combined with carboplatin and paclitaxel in chemotherapy-naive patients with advanced non-small cell lung cancer. j thorac oncol. 2012 feb;7(2):427-33.

Orantinib (SU6668) Preparation Products And Raw materials

Raw materials

Preparation Products

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Orantinib (SU6668) Suppliers

Novachemistry
Tel
44-20819178-90 02081917890
Fax
(0)2080432064
Email
info@novachemistry.com
Country
United Kingdom
ProdList
4381
Advantage
58
Tocris Bioscience
Tel
--
Fax
--
Email
customerservice@tocris.co.uk
Country
United Kingdom
ProdList
5726
Advantage
77
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View Lastest Price from Orantinib (SU6668) manufacturers

Career Henan Chemical Co
Product
3-[2,4-dimethyl-5-[(E)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid 252916-29-3
Price
US $1.00/KG
Min. Order
1G
Purity
99%
Supply Ability
100KG
Release date
2018-08-13

252916-29-3, Orantinib (SU6668)Related Search:


  • 3-[2,4-dimethyl-5-[(E)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid
  • TSU-68
  • 5-[1,2-Dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-propanoic acid
  • (Z)-3-(2,4-dimethyl-5-((2-oxoindolin-3-ylidene)methyl)-1H-pyrrol-3-yl)propanoic acid
  • TSU-68 (SU6668)
  • 1H-Pyrrole-3-propanoic acid, 5-[(1,2-dihydro-2-oxo-3H-indol-3-ylidene)Methyl]-2,4-diMethyl-
  • SU 6668(TSU-68)
  • (E)-3-(2,4-diMethyl-5-((2-oxoindolin-3-ylidene)Methyl)-1H-pyrrol-3-yl)propanoic acid
  • NSC 702827
  • TSU-68 (SU6668, Orantinib)
  • Orantinib
  • 3-(2,4-DiMethyl-5-((2-oxoindolin-3-ylidene)Methyl)-1H-pyrrol-3-yl)propanoic acid
  • 5-[1,2-Dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-propanoic acid TSU-68 (SU6668, Orantinib)
  • TSU-68, >=99%
  • 3-[2,4-dimethyl-5-[(E)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid TSU-68
  • (Z)-3-[2,4-Dimethyl-5-(2-oxo-2,3-dihydro-1H-indol-3-ylidenemethyl)-1H-pyrrol-3-yl]propionic acid
  • TSU-68 (SU6668, ORANTINIB);SU 6668;TSU68
  • ORANTINIB;SU6668;SU 6668;NSC 702827
  • Orantinib (SU6668
  • ORANTINIB (SU6668; TSU-68)
  • Orantinib (TSU-68)
  • TSU-68;SU6668; NSC 702827;TSU 68;TSU68
  • TSU-68 (Orantinib,SU6668)
  • Orantinib (TSU-68, SU6668)
  • Orantinib (SU6668) USP/EP/BP
  • Orantinib SU6668 PDGFR inhibitor ab142156 SU-6668 tsu68 tsu-68
  • Orantinib (SU
  • 252916-29-3
  • API
  • Angiogenesis and Metastasis
  • Inhibitors