WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H406791
CAS#: 867331-82-6 (free base)
Description: TG100801 or TG-100801 is a dual inhibitor of both VEGFr2 and the Src family (Src and YES) kinases as a topically administered therapeutic candidate in clinical trials for the treatment of age-related macular degeneration. TG100801 is a multi-kinases inhibitor. It is a pro-drug version of TG100572. Age-related macular degeneration (AMD) is the leading cause of blindness in the Western world for those patients aged 50 years or older.
Hodoodo Cat#: H406791
Name: TG100801
CAS#: 867331-82-6 (free base)
Chemical Formula: C33H30ClN5O3
Exact Mass: 579.20
Molecular Weight: 580.085
Elemental Analysis: C, 68.33; H, 5.21; Cl, 6.11; N, 12.07; O, 8.27
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Related CAS #: 867331-82-6 (free base) 1018069-81-2 (HCl)
Synonym: TG100801; TG-100801; TG 100801.
IUPAC/Chemical Name: 4-chloro-3-(5-methyl-3-((4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)amino)benzo[e][1,2,4]triazin-7-yl)phenyl benzoate
InChi Key: JMGXJHWTVBGOKG-UHFFFAOYSA-N
InChi Code: InChI=1S/C33H30ClN5O3/c1-22-19-24(28-21-27(13-14-29(28)34)42-32(40)23-7-3-2-4-8-23)20-30-31(22)36-33(38-37-30)35-25-9-11-26(12-10-25)41-18-17-39-15-5-6-16-39/h2-4,7-14,19-21H,5-6,15-18H2,1H3,(H,35,36,38)
SMILES Code: CC1=C2C(=CC(=C1)C3=C(C=CC(=C3)OC(=O)C4=CC=CC=C4)Cl)N=NC(=N2)NC5=CC=C(C=C5)OCCN6CCCC6
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
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The following data is based on the product molecular weight 580.09 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Sharma S, Mulik S, Kumar N, Suryawanshi A, Rouse BT. An anti-inflammatory role of VEGFR2/Src kinase inhibitor in herpes simplex virus 1-induced immunopathology. J Virol. 2011 Jun;85(12):5995-6007. doi: 10.1128/JVI.00034-11. Epub 2011 Apr 6. PubMed PMID: 21471229; PubMed Central PMCID: PMC3126288.
2: Ni Z, Hui P. Emerging pharmacologic therapies for wet age-related macular degeneration. Ophthalmologica. 2009;223(6):401-10. doi: 10.1159/000228926. Epub 2009 Jul 20. Review. PubMed PMID: 19622904.
3: Barakat MR, Kaiser PK. VEGF inhibitors for the treatment of neovascular age-related macular degeneration. Expert Opin Investig Drugs. 2009 May;18(5):637-46. doi: 10.1517/13543780902855316 . Review. PubMed PMID: 19388880.
4: Palanki MS, Cao J, Chow CP, Dneprovskaia E, Mak CC, McPherson A, Pathak VP, Renick J, Soll R, Zeng B, Noronha G. Development of novel benzotriazines for drug discovery. Expert Opin Drug Discov. 2009 Jan;4(1):33-49. doi: 10.1517/17460440802580536. Epub 2008 Dec 10. PubMed PMID: 23480335.
5: Chappelow AV, Kaiser PK. Neovascular age-related macular degeneration: potential therapies. Drugs. 2008;68(8):1029-36. Review. PubMed PMID: 18484796.
6: Doukas J, Mahesh S, Umeda N, Kachi S, Akiyama H, Yokoi K, Cao J, Chen Z, Dellamary L, Tam B, Racanelli-Layton A, Hood J, Martin M, Noronha G, Soll R, Campochiaro PA. Topical administration of a multi-targeted kinase inhibitor suppresses choroidal neovascularization and retinal edema. J Cell Physiol. 2008 Jul;216(1):29-37. doi: 10.1002/jcp.21426. PubMed PMID: 18330892; PubMed Central PMCID: PMC3032767.
7: Palanki MS, Akiyama H, Campochiaro P, Cao J, Chow CP, Dellamary L, Doukas J, Fine R, Gritzen C, Hood JD, Hu S, Kachi S, Kang X, Klebansky B, Kousba A, Lohse D, Mak CC, Martin M, McPherson A, Pathak VP, Renick J, Soll R, Umeda N, Yee S, Yokoi K, Zeng B, Zhu H, Noronha G. Development of prodrug 4-chloro-3-(5-methyl-3-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}-1,2,4-benzotria zin-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. doi: 10.1021/jm7011276. Epub 2008 Feb 27. PubMed PMID: 18311895.
