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TG 100801

CAT: 0804-HY-10186-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-10186-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
TG 100801 is a proagent that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
CAS Number
867331-82-6
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
FGFR; PDGFR; Src; VEGFR
Type
Reference compound
Related Pathways
Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/TG-100801.html
Purity
98.61
Solubility
DMSO : 5.56 mg/mL (ultrasonic)
Smiles
O=C(C1=CC=CC=C1)OC2=CC=C(Cl)C(C3=CC(C)=C(N=C(NC(C=C4)=CC=C4OCCN5CCCC5)N=N6)C6=C3)=C2
Molecular Formula
C33H30ClN5O3
Molecular Weight
580.08
Precautions
H302, H315, H319, H335
References & Citations
[1]Palanki MS, et al. Development of prodrug 4-chloro-3- (5-methyl-3-{[4- (2-pyrrolidin-1-ylethoxy) phenyl]amino}-1,2,4-benzotriazin-7-yl) phenyl benzoate (TG100801) : a topically administered therapeutic candidate in clinical trials for the treatment of age-related macular degeneration. J Med Chem. 2008 Mar 27;51 (6) :1546-59.|[2]Doukas, John, et al. Topical administration of a multi-targeted kinase inhibitor suppresses choroidal neovascularization and retinal edema. Journal of Cellular Physiology (2008), 216 (1), 29-37.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
PDGFRβ; VEGFR1/Flt-1; VEGFR2/KDR/Flk-1

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