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MedKoo Cat#: 406791 | Name: TG100801

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

TG100801
TG100801
CAS#867331-82-6 (free base)

Theoretical Analysis

MedKoo Cat#: 406791

Name: TG100801

CAS#: 867331-82-6 (free base)

Chemical Formula: C33H30ClN5O3

Exact Mass: 579.2037

Molecular Weight: 580.09

Elemental Analysis: C, 68.33; H, 5.21; Cl, 6.11; N, 12.07; O, 8.27

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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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

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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
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.