Orantinib (SU6668)
- Product Name
- Orantinib (SU6668)
- CAS No.
- 252916-29-3
- Chemical Name
- Orantinib (SU6668)
- Synonyms
- TSU-68;Orantinib;NSC 702827;TSU-68, >=99%;TSU-68 (SU6668);SU 6668(TSU-68);Orantinib (SU6668;Orantinib (TSU-68);TSU-68 (Orantinib,SU6668);TSU-68 (SU6668, Orantinib)
- CBNumber
- CB31456201
- Molecular Formula
- C18H18N2O3
- Formula Weight
- 310.35
- MOL File
- 252916-29-3.mol
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
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..…
N-Bromosuccinimide Price
- Product number
- 13873
- Product name
- SU 6668
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $31
- Updated
- 2024/03/01
- Product number
- 13873
- Product name
- SU 6668
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $73
- Updated
- 2024/03/01
- Product number
- 13873
- Product name
- SU 6668
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $121
- Updated
- 2024/03/01
- Product number
- 022488
- Product name
- TSU-68
- Packaging
- 10mg
- Price
- $396
- Updated
- 2021/12/16
- Product number
- T797550
- Product name
- TSU-68
- Packaging
- 50mg
- Price
- $425
- Updated
- 2021/12/16
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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View Lastest Price from Orantinib (SU6668) manufacturers
- 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