2. Protein Tyrosine Kinase/RTK
  3. Src VEGFR PDGFR FGFR
  4. TG 100572

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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (TG 100572 Hydrochloride) usually boasts enhanced water solubility and stability.

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

TG 100572 Chemical Structure

TG 100572 Chemical Structure

CAS No. : 867334-05-2

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TG 100572 Related Antibodies

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FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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.

IC50 & Target[1]

VEGFR1

2 nM (IC50)

VEGFR2

7 nM (IC50)

FGFR1

2 nM (IC50)

FGFR2

16 nM (IC50)

PDGFRβ

13 nM (IC50)

In Vitro

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[1]. TG 100572 is shown to inhibit hRMVEC cell proliferation, with an IC50 of 610±72 nM. This suggests that TG 100572 has the therapeutic potential to inhibit VEGF function in ocular endothelial cells, a contributing factor to pathological angiogenesis in diseases such as AMD and PDR[2].

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

TG 100572 Related Antibodies
In Vivo

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[1]. 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[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

475.97

Formula

C26H26ClN5O2
CAS No.
SMILES

ClC1=CC=C(O)C=C1C2=CC(C)=C(N=C(NC(C=C3)=CC=C3OCCN4CCCC4)N=N5)C5=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro: 

DMSO : ≥ 150 mg/mL (315.15 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1010 mL 10.5049 mL 21.0097 mL
5 mM 0.4202 mL 2.1010 mL 4.2019 mL
View the Complete Stock Solution Preparation Table

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References
Cell Assay
[1]

For proliferation assays, human retinal microvascular EC plated in 96-well cluster plates are cultured for 48 hr in the presence of either TG 100572 (2 nM-5 µM) or DMSO; medium contained 10% FBS, 50 µg/mL heparin, and 50 ng/mL rhVEGF. Cell numbers are then assessed using an XTT-based assay[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice: C57BL/6 mice (15-20 g) are dosed i.p. twice daily for 4 days with 5 mg/ kg TG 100572, followed by a single dose on Day 5, 5 hr after which plasma samples are taken, animals euthanized, and eyes explanted. Alternatively, mice are dosed topically with either TG 100572 or related prodrugs (e.g., TG 100801) by delivering a single 10 µL drop to both eyes for a total of two days, and both plasma and eyes harvested prior to or 0.5, 1, 3, 5, or 7 hr after the Day 2 dosing[1].

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

Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1010 mL 10.5049 mL 21.0097 mL 52.5243 mL
5 mM 0.4202 mL 2.1010 mL 4.2019 mL 10.5049 mL
10 mM 0.2101 mL 1.0505 mL 2.1010 mL 5.2524 mL
15 mM 0.1401 mL 0.7003 mL 1.4006 mL 3.5016 mL
20 mM 0.1050 mL 0.5252 mL 1.0505 mL 2.6262 mL
25 mM 0.0840 mL 0.4202 mL 0.8404 mL 2.1010 mL
30 mM 0.0700 mL 0.3502 mL 0.7003 mL 1.7508 mL
40 mM 0.0525 mL 0.2626 mL 0.5252 mL 1.3131 mL
50 mM 0.0420 mL 0.2101 mL 0.4202 mL 1.0505 mL
60 mM 0.0350 mL 0.1751 mL 0.3502 mL 0.8754 mL
80 mM 0.0263 mL 0.1313 mL 0.2626 mL 0.6566 mL
100 mM 0.0210 mL 0.1050 mL 0.2101 mL 0.5252 mL
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TG 100572 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TG 100572867334-05-2TG100572TG-100572SrcVEGFRPDGFRFGFRVascular endothelial growth factor receptorPlatelet-derived growth factor receptorFibroblast growth factor receptorInhibitorinhibitorinhibit

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