1. Protein Tyrosine Kinase/RTK
  2. VEGFR
    FGFR
    PDGFR
    Src
  3. TG 100801

TG 100801 

Cat. No.: HY-10186 Purity: 98.60%
Handling Instructions

TG 100801 is a prodrug 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 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.

For research use only. We do not sell to patients.

TG 100801 Chemical Structure

TG 100801 Chemical Structure

CAS No. : 867331-82-6

Size Price Stock Quantity
5 mg USD 264 In-stock
Estimated Time of Arrival: December 31
10 mg USD 456 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1152 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of TG 100801:

Top Publications Citing Use of Products

Publications Citing Use of MCE TG 100801

View All VEGFR Isoform Specific Products:

View All FGFR Isoform Specific Products:

View All PDGFR Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

TG 100801 is a prodrug 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 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.

IC50 & Target

IC50: 2 nM (VEGFR1), 7 nM (VEGFR2), 2 nM (FGFR1), 16 nM (FGFR2), 13 nM (PDGFRβ), 5 nM (Fgr), 0.5 nM (Fyn), 6 nM (Hck), 0.1 nM (Lck), 0.4 nM (Lyn), 1 nM (Src), 0.2 nM (Yes)[1]

In Vitro

TG 100801 is a topically administered prodrug delivered as an eye drop that is readily converted to the active TG 100572 in the eye.TG 100572 is shown to inhibit hRMVEC cell proliferation, with an IC50 of 610±72 nM[1]. TG 100801 is formed by derivitization of a phenolic moiety in TG100572 to yield an ester. It displays excellent balance of stability (physical and chemical) with hydrolysis rate. On its own, TG 100801 does not display meaningful anti-kinase activity, as the ester group blocks key interactions with kinase active sites, however exposure to esterases (abundant in mammalian tissues) rapidly liberates active TG100572.TG 100572 shows sub-nanomolar activity against the Src family as well as RTK such as VEGFR1 and R2, FGFR1 and R2, and PDGFRβ. TG 100572 inhibits vascular endothelial cell proliferation (ED50=610±71 nM) and blocks VEGF-induced phosphorylation of extracellular signal-regulated kinase. TG 100572 induces apoptosis in rapidly proliferating, but not quiescent, endothelial cell cultures[2].

In Vivo

TG 100801 exhibits excellent ocular pharmacokinetics and poor systemic circulation and shows good efficacy in the laser induced choroidal neovascularization model. A concentration of 23.4 µM (Cmax) of TG 100572 is reached in 30 min (Tmax)=0.5 h) in the choroid and the sclera. However, the levels of TG 100572 in the retina are relatively low. The half-life of TG 100572 in ocular tissues is very short; hence, the compound is administered topically minimum t.i.d. to maintain appropriate drug levels in the eye. The maximum concentration one can achieve in formulations using TG 100572 is 0.7% w/v[1]. TG 100801 nor TG100572 are detectable in plasma following topical delivery of TG 100801, and adverse safety signals (such as weight loss) are not observed even with prolonged dosing schedules. Topical TG 100801 significantly suppresses laser-induced choroidal neovascularlization in mice, and reduces fluorescein leakage from the vasculature and retinal thickening measured by optical coherence tomography in a rat model or retinal vein occlusion.Systemic delivery of TG 100572 in a murine model of laser-induced choroidal neovascularization (CNV) causes significant suppression of CNV, but with an associated weight loss suggestive of systemic toxicity[2].

Clinical Trial
Molecular Weight

580.08

Formula

C₃₃H₃₀ClN₅O₃

CAS No.

867331-82-6

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5.56 mg/mL (9.58 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7239 mL 8.6195 mL 17.2390 mL
5 mM 0.3448 mL 1.7239 mL 3.4478 mL
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[2]

Rats: Long Evans rats are dosed topically in both eyes with 10 µL of TG 100801 (as a 0.3, 0.6 or 1% solution) or vehicle. A total of 5 topical applications are delivered per eye over a three day period: dosing is performed one hour prior to and six hours after laser-induced thrombosis on Day 1, twice on Day 2, and once the morning of Day 3. One hour after the final topical application, retinal edema is assessed by one of two means[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 98.60%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

TG 100801TG100801TG-100801VEGFRFGFRPDGFRSrcVascular endothelial growth factor receptorFibroblast growth factor receptorPlatelet-derived growth factor receptorInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
TG 100801
Cat. No.:
HY-10186
Quantity:
MCE Japan Authorized Agent: