[CAS NO. 1191450-19-7] Burixaforhydrobromide
PRODUCTS SPECIFICATIONS [1191450-19-7]
DESCRIPTION [1191450-19-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 769.01 |
| Molecular Formula | C27H51N8O3P.5/2HBr |
| SMILES | NC1=CC(N2CCN(CCP(O)(O)=O)CC2)=NC(NC[C@H]3CC[C@H](CNCCCNC4CCCCC4)CC3)=N1.[H]Br.[5/2] |
Summary
Burixafor hydrobromide (TG-0054 hydrobromide) is an orally bioavailable and potent antagonist of CXCR4 and a well anti-angiogenic drug that is of potential value in treating choroid neovascularization [1] . Burixafor hydrobromide (TG-0054 hydrobromide) mobilizes mesenchymal stem cells, attenuates inflammation, and preserves cardiac systolic function in a porcine model of myocardial infarction [2] .
IC50 & Target
|
CXCR4 |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01018979 | GPCR Therapeutics, Inc. |
Multiple Myeloma|Non-Hodgkin Lymphoma|Hodgkin Disease
|
February 2010 | Phase 2 |
| NCT02104427 | GPCR Therapeutics, Inc. |
Multiple Myeloma|Non-Hodgkin Lymphoma|Hodgkin Disease
|
February 2015 | Phase 2 |
| NCT01458288 | GPCR Therapeutics, Inc. |
Multiple Myeloma|Non-hodgkin´s Lymphoma|Hodgkin´s Disease
|
October 2012 | Phase 2 |
| NCT00822341 | GPCR Therapeutics, Inc. |
Healthy
|
April 2008 | Phase 1 |
| NCT02478125 | Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Prostate Cancer Foundation|TaiGen Biotechnology Co., Ltd. |
Prostate Cancer
|
July 2016 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
H 2 O : 50 mg/mL ( 65.02 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.3004 mL | 6.5019 mL | 13.0037 mL |
| 5 mM | 0.2601 mL | 1.3004 mL | 2.6007 mL |
| 10 mM | 0.1300 mL | 0.6502 mL | 1.3004 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 20 mg/mL (26.01 mM); Clear solution; Need ultrasonic
References
- [1] Shelke NB, et al. Intravitreal Poly(L-lactide) Microparticles Sustain Retinal and Choroidal Delivery of TG-0054, a Hydrophilic Drug Intended for Neovascular Diseases. Drug Deliv Transl Res. 2011 Feb;1(1):76-90.
- [2] Hsu WT, et al. CXCR4 Antagonist TG-0054 Mobilizes Mesenchymal Stem Cells, Attenuates Inflammation, and Preserves Cardiac Systolic Function in a Porcine Model of Myocardial Infarction. Cell Transplant. 2015;24(7):1313-28.
