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> Pathway Inhibitors>Protein Inhibitors>AXT107 (Gersizangitide)

Protein Inhibitors

AXT107 View larger

AXT107 (Gersizangitide)

AOB13608

Chemical Name: 

Gersizangitide; SP2043; LRRFSTAPFAFIDINDVINF; Leu-Arg-Arg-Phe-Ser-Thr-Ala-Pro-Phe-Ala-Phe-Ile-Asp-Ile-Asn-Asp-Val-Ile-Asn-Phe 3 TFA salt

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Quantity Discount Table - Order More To Get More Price Discount

QuantitymgUnit Price ($/mg or $/Unit)Final Price
15 $24.65 Total: $123.25
110 $20.88 Total: $208.80
125 $17.69 Total: $442.25
150 $15.08 Total: $754.00
1100 $13.05 Total: $1,305.00

Data sheet

Molecular FormulaC117H169F9N28O35
Molecular Weight2698.79
CAS Numbers2417491-82-6
Storage Condition0°C (short term), -20°C (long term), desiccated
SolubilityDMSO
Purity98% by HPLC
SynonymGersizangitide; SP2043; LRRFSTAPFAFIDINDVINF; Leu-Arg-Arg-Phe-Ser-Thr-Ala-Pro-Phe-Ala-Phe-Ile-Asp-Ile-Asn-Asp-Val-Ile-Asn-Phe 3 TFA salt
IUPAC/Chemical NameLRRFSTAPFAFIDINDVINF; Leu-Arg-Arg-Phe-Ser-Thr-Ala-Pro-Phe-Ala-Phe-Ile-Asp-Ile-Asn-Asp-Val-Ile-Asn-Phe 3 TFA salt
InChl KeyYVOJSNXOGANXSQ-BZHNYRKKSA-N
InChl CodeInChI=1S/C111H167N29O28/c1-14-58(8)86(105(164)132-76(52-82(114)144)98(157)129-77(53-83(145)146)100(159)135-85(57(6)7)104(163)138-88(60(10)16-3)107(166)131-75(51-81(113)143)97(156)126-71(90(115)149)47-64-32-21-17-22-33-64)137-101(160)78(54-84(147)148)133-106(165)87(59(9)15-2)136-99(158)74(50-67-38-27-20-28-39-67)127-91(150)61(11)122-95(154)72(48-65-34-23-18-24-35-65)130-103(162)80-42-31-45-140(80)109(168)62(12)123-108(167)89(63(13)142)139-102(161)79(55-141)134-96(155)73(49-66-36-25-19-26-37-66)128-94(153)70(41-30-44-121-111(118)119)125-93(152)69(40-29-43-120-110(116)117)124-92(151)68(112)46-56(4)5/h17-28,32-39,56-63,68-80,85-89,141-142H,14-16,29-31,40-55,112H2,1-13H3,(H2,113,143)(H2,114,144)(H2,115,149)(H,122,154)(H,123,167)(H,124,151)(H,125,152)(H,126,156)(H,127,150)(H,128,153)(H,129,157)(H,130,162)(H,131,166)(H,132,164)(H,133,165)(H,134,155)(H,135,159)(H,136,158)(H,137,160)(H,138,163)(H,139,161)(H,145,146)(H,147,148)(H4,116,117,120)(H4,118,119,121)/t58-,59-,60-,61-,62-,63+,68-,69-,70-,71-,72-,73-,74-,75-,76-,77-,78-,79-,80-,85-,86-,87-,88-,89-/m0/s1
SMILES CodeCC[C@H](C)[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N)NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](C)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@@H]4CCCN4C(=O)[C@H](C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC5=CC=CC=C5)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)N
References1) Fei X, et al. Challenges and opportunities of developing small-molecule therapies for age-related macular degeneration. Arch Pharm Res. 2024 Jun;47(6):538-557.

2) Mirando AC, et al. A collagen IV-derived peptide disrupts α5β1 integrin and potentiates Ang2/Tie2 signaling. JCI Insight. 2019 Feb 21;4(4):e122043. [Content Brief]

More info

Type IV collagen-derived peptide, inhibiting the activation of multiple growth factor receptors, including many related to both angiogenesis and lymphangiogensis (ie. VEGFR2 and VEGFR3), inhibiting the growth of a primary triple negative breast cancer (TNBC) tumor xenograft and its metastasis to the lungs and lymph nodes by blocking lymphangiogenesis and angiogenesis in pre-metastatic organs as well as primary tumors

Mechanism of Action / Functional Effects

AXT107 has a dual (or multi-modal) mechanism that acts on several pathways involved in angiogenesis, vascular stability, and permeability. Key functional effects include:

Target / PathwayEffect of AXT107Functional Consequence
Integrins α_vβ_3 and α_5β_1AXT107 binds these integrins with high affinity and disrupts their interaction with extracellular matrix. IOVS+4Cell+4PMC+4This integrin binding helps localize AXT107 to diseased vasculature and modulates downstream signaling.
VEGF Receptor Signaling (especially VEGFR2)It inhibits or blocks signaling through VEGF receptors (e.g., VEGFR2) Synapse+5IOVS+5aobious.com+5Suppression of pro-angiogenic signaling — reduces new blood vessel formation (neovascularization) and leakage.
Tie2 Pathway ActivationAXT107 promotes or enables activation of Tie2 (the TEK receptor tyrosine kinase) by facilitating Ang2 (or angiopoietin) interactions under certain conditions. Cell+3IOVS+3Ophthalmology Times+3Tie2 activation contributes to vascular stabilization, reduced permeability, and anti-inflammatory effects.
Vascular Permeability / LeakageAXT107 has “antipermeability” activity (i.e. it reduces vascular leakage) in models of ischemic retinopathy. IOVS+3PMC+3Hopkins Medicine+3This is critical in retinal diseases where fluid leakage causes edema and vision impairment.
Neovascularization / AngiogenesisIt suppresses abnormal vessel growth (neovascularization) in ocular models. aobious.com+4IOVS+4Cell+4Helps prevent or regress pathological new vessel formation in retinal diseases.
Anti-inflammatory effectsIt appears to suppress inflammatory processes in the vascular environment. Hopkins Medicine+3Ophthalmology Times+3IOVS+3Inflammation often accompanies vascular leakage and neovascular disease, so this helps in limiting damage.

In sum, AXT107 is designed to both block pro-angiogenic (VEGF) signals and promote vascular stabilization (via Tie2 activation), making it a promising candidate for treating vascular disorders in the retina where leakage and pathological vessel growth are central to disease. aobious.com+3IOVS+3Ophthalmology Times+3

Preclinical / Clinical Considerations

  • In animal models, AXT107, when injected intraocularly, was shown to localize to areas of abnormal vessels (where integrins are upregulated) and reduce vascular leakage. PMC+2Hopkins Medicine+2

  • Because AXT107 is poorly soluble, formulations may form a gel or microparticulate suspension in the vitreous, allowing for sustained release. HCPLive+2Ophthalmology Times+2

  • Some preclinical and early clinical data suggest that a single intraocular injection of AXT107 may sustain effects over extended periods (potentially reducing treatment burden). HCPLive+2Ophthalmology Times+2

  • It is currently in Phase I/II trials for neovascular age-related macular degeneration (nAMD) via suprachoroidal injection. aobious.com+3Synapse+3Ophthalmology Times+3