Synonym |
LY2510924 |
Species |
Human |
Protein Accession |
Q14529 |
Purity |
Greater than 95% as determined by SDS-PAGE |
Endotoxin Level |
Less than 1 EU/µg |
Biological Activity |
The ED50 for this effect is typically 3-15 μg/mL |
Expression System |
Baculovirus |
Fusion Tag |
C-6His |
Predicted Molecular Mass |
39.1 kDa |
Formulation |
Lyophilized from a 0.2 μm filtered solution in PBS |
Reconstitution |
Centrifuge the vial prior to opening. Reconstitute in PBS to a concentration of 0.1-1.0 mg/mL
|
Storage & Stability |
Store at -20°C. Store under sterile conditions at -20°C, -80°C or at lower temperature. It is
recommended to reconstitute the lyophilized product in sterile distilled water or aqueous buffer
containing 0.1% BSA. |
FAQ
What is LY2510924, and what makes it unique as a therapeutic solution?
LY2510924 is a specialized
compound designed as a CXCR4 antagonist, which means it is uniquely positioned to inhibit the CXCR4
receptor pathway. The CXCR4 receptor is part of the chemokine receptor family and plays a significant
role in various physiological and pathological processes such as the immune response, inflammation, and
tumor progression. What sets LY2510924 apart as a therapeutic solution is its selective targeting
capability. The precision of LY2510924 in targeting the CXCR4 receptor helps minimize the potential for
off-target effects, which is a common limitation with many therapeutic agents. This focus ensures that
the intended therapeutic pathways are modulated with minimal interference in other physiological
processes. Furthermore, LY2510924's potency as a CXCR4 antagonist showcases its potential in disrupting
CXCL12-CXCR4 interactions. These interactions are crucial in many pathological processes, notably in
cancer metastasis, where the CXCR4 receptor and its ligand CXCL12 facilitate the migration and invasion
of cancer cells. By interfering in this pathway, LY2510924 provides a mechanism to potentially reduce
tumor growth and metastasis without affecting the normal functions regulated by different chemokine
pathways. Additionally, the unique pharmacokinetic profile of LY2510924 contributes to its efficacy and
safety profile, highlighting its promise as a long-lasting therapeutic intervention. Research studies
have shown that LY2510924 has a satisfactory safety profile in clinical trials, indicating a favorable
balance between its therapeutic efficacy and potential adverse effects. The combination of its targeted
action, therapeutic potential, and safety profile makes LY2510924 a promising candidate in medical
research, especially in fields that deal with complex diseases like cancer and certain immune disorders,
where CXCR4 is implicated.
How does LY2510924 function, and what are its potential therapeutic
applications?
LY2510924 functions primarily as a CXCR4 receptor antagonist. CXCR4 is a part of
the chemokine receptor family and, in synergy with its ligand CXCL12 (also known as stromal cell-derived
factor-1), plays crucial roles in several biological processes, including stem cell trafficking and
cancer cell metastasis. The primary mechanism by which LY2510924 exerts its function is by competitively
binding to the CXCR4 receptor, thus inhibiting the interaction between CXCR4 and CXCL12. This blockade
limits the downstream signaling pathways activated by this receptor-ligand duo, primarily the PI3K/Akt
and MAPK pathways, known for their roles in cell survival, proliferation, and migration. By specifically
targeting these signaling pathways, LY2510924 effectively modulates processes that are critical for the
progression of certain diseases, making its therapeutic applications broad and promising. In cancer
therapy, LY2510924's potential to inhibit tumor growth and metastasis is particularly significant. The
CXCL12/CXCR4 axis is vital for the homing and migration of cancer cells to distant organs. Thus,
LY2510924 can be used in therapeutic strategies aimed at preventing cancer dissemination and potentially
enhancing the effectiveness of standard treatments like chemotherapy by making cancer cells more
susceptible to cytotoxic agents. Besides oncology, LY2510924 may also have therapeutic applications in
treating AIDS. The CXCR4 receptor is one of the co-receptors exploited by HIV to gain entry into CD4+
T-cells. By blocking CXCR4, LY2510924 could potentially inhibit HIV progression in patients who have
highly resistant forms of the virus, thereby serving as an adjuvant to existing antiretroviral
therapies. Furthermore, LY2510924 might have potential applications in regenerative medicine, especially
where enhancing or inhibiting certain stem cell processes is beneficial. By modulating the CXCL12/CXCR4
axis, LY2510924 can influence stem cell mobilization and homing, which are critical in regenerative
processes. Therefore, while still primarily investigated within oncology, LY2510924's broad mechanism of
action offers hope across various fields of medicine.
What are the current research findings
regarding LY2510924’s effectiveness and safety profile?
Recent research findings on LY2510924
have provided valuable insights into its effectiveness and safety profile, forming a promising outlook
for its potential therapeutic applications. Effectiveness studies have primarily centered around
LY2510924’s role in oncology, where the CXCL12/CXCR4 axis is a well-known facilitator of tumor
proliferation and metastasis. Preclinical studies using animal models have demonstrated that LY2510924
can significantly impede tumor growth in various cancer types, including breast and prostate cancers.
These animal models, which closely mimic the human disease profile, have shown reduced tumor spread and
increased sensitivity to conventional chemotherapeutic agents when LY2510924 is introduced. Moreover, in
vitro studies with cancer cell lines have further corroborated these findings by showing reduced
migratory and invasive capabilities of cancer cells upon treatment with LY2510924. Safety, on the other
hand, is a critical aspect assessed in various clinical phase trials. LY2510924 has undergone several
early-phase human clinical trials, with results indicating a generally favorable safety profile. In
these studies, LY2510924 was administered to participants at different dosages to determine tolerability
and identify any potential adverse effects. The majority of adverse effects were mild to moderate in
nature, with the most common being temporary injection site reactions, mild gastrointestinal symptoms,
and occasional flu-like symptoms. Importantly, no dose-limiting toxicities were observed, allowing
researchers to establish a feasible therapeutic range. This safety data is extremely pertinent, given
the drug’s potential application in a broad range of patients, some of whom might have limited tolerance
for adverse effects due to existing conditions. Expanding on the clinical findings, pharmacokinetic
studies of LY2510924 have shown promising results in terms of drug metabolism and excretion. The
compound exhibits a half-life conducive to sustained therapeutic action with manageable dosing
intervals, which is an advantageous property for patient compliance. Present datasets from these
early-phase trials provide a foundation for more extensive studies aimed at optimizing dosage regimens
and further evaluating long-term safety. In particular, ongoing trials are exploring combination
therapies, where LY2510924 is paired with existing cancer treatments, which could highlight synergies
that enhance overall treatment efficacy. While more research is necessary to fully elucidate LY2510924's
mechanism, the existing data underscores its potential as both a monotherapy and part of combination
therapies.
How does LY2510924 compare to other CXCR4 antagonists on the market?
LY2510924
represents a class of compounds specifically engineered to target and inhibit the CXCR4 receptor. When
comparing LY2510924 to other CXCR4 antagonists available in the market, some distinguishing features
become apparent, which may present LY2510924 as a potential superior alternative under certain
conditions. Firstly, a notable aspect of LY2510924 is its high specificity and binding affinity for the
CXCR4 receptor. This feature is crucial because it reduces the probability of off-target effects, which
can lead to unintended side effects. Many other CXCR4 antagonists may not offer the same level of
specificity, potentially increasing risks associated with broader receptor inhibition. High specificity
is especially valuable in cancer therapies, where precision targeting can significantly impact the
effectiveness and safety of the treatment. In comparison to polypharmacological agents that interact
with multiple receptors, LY2510924’s focused action presents a more targeted approach, thus minimizing
interactions with non-CXCR4 mediated pathways. Another major advantage of LY2510924 is its promising
safety and tolerability profile as observed in clinical evaluations. While many CXCR4 antagonists are
effective, they often come with a spectrum of side effects ranging from mild to severe, which can impair
patient quality of life and adherence to treatment regimens. LY2510924 shows a trend towards a lower
incidence of adverse effects, which can be a critical determinant in its acceptability against other
treatment options. Furthermore, LY2510924’s long half-life and ease of dosing contribute to its
comparability. As a therapeutic agent, having a longer half-life generally allows for less frequent
dosing, which enhances patient compliance, especially in chronic conditions requiring long-term
management. Many existing CXCR4 antagonists might require more frequent administration, adding to
treatment burden for patients. The pharmacokinetic characteristics of LY2510924, combined with its human
trial data, suggest it is a convenient option in terms of dosing and patient adherence. Moreover,
research is actively exploring the use of LY2510924 in diverse applications, including combinational
therapy with other cancer treatments and potential applications in HIV management. This versatility is
indicative of a compound poised to be a valuable asset in therapeutic options, potentially outshining
other CXCR4 antagonists that may have narrower applications. While LY2510924 is one of several agents
targeting the CXCR4 receptor, its unique pharmacological profile and early trial results suggest it
could offer advantages in targeting specific diseases, such as certain types of cancer and immune
disorders. As ongoing research continues to examine its full potential, LY2510924 stands out in the
competitive landscape of CXCR4 antagonism.
What potential side effects and contraindications have
been identified with LY2510924 use?
As with any therapeutic agent, understanding the potential
side effects and contraindications of LY2510924 is essential for its safe and effective application in
clinical settings. LY2510924 has undergone various phases of clinical trials to evaluate its safety
profile, with a focus on identifying and categorizing any adverse effects associated with its
administration. Through these trials, several potential side effects have been documented, most of which
are manageable and typically transient in nature. The most frequently reported side effects of LY2510924
include mild to moderate injection site reactions. These reactions usually manifest as redness,
swelling, or discomfort at the injection site, resolving within a few days without the need for medical
intervention. Additionally, some patients have reported experiencing flu-like symptoms, such as
headache, fatigue, and mild fever, particularly following initial doses as the body adjusts to the
treatment. Gastrointestinal symptoms such as nausea and diarrhea have also been observed, although these
are generally self-limiting and treated with over-the-counter medications. From a contraindication
standpoint, LY2510924 use should be approached with caution in specific patient populations. Individuals
with a known hypersensitivity to LY2510924 or any of its constituents are advised against its use. It is
also important to consider the immunomodulatory effects of LY2510924, particularly in patients with
compromised immune systems or those undergoing immunosuppressive therapies. The CXCR4 receptor plays a
role in the immune system; thus, its antagonism could potentially exacerbate immunosuppression in these
patients, increasing their susceptibility to infections. Pregnant or breastfeeding women are advised to
evaluate the risks and benefits of undergoing treatment with LY2510924, as there is limited data on its
effects during pregnancy or lactation. Animal studies have provided some insights, but human data is
still lacking, warranting a cautious approach. Additionally, elderly patients or those with existing
co-morbidities should be carefully evaluated to ensure that LY2510924 does not interact adversely with
their current medications or underlying health conditions. Contradictory outcomes might arise where
LY2510924's use interferes with the effectiveness of drugs metabolized through similar pathways or where
it exacerbates pre-existing conditions. Healthcare professionals are encouraged to conduct thorough
evaluations and consider medical history before initiating LY2510924 therapy. Overall, while LY2510924
demonstrates a relatively benign side effect profile, understanding these aspects is crucial in
maximizing its therapeutic benefits while minimizing potential risks.
What are the major
challenges and future prospects for the development and application of LY2510924?
The development
and application of LY2510924 are promising fields with exciting opportunities, yet they bring some
challenges that need to be addressed to pave the way for broader use in clinical settings. One of the
key challenges in LY2510924 development lies in comprehensively understanding its long-term effects.
Most of the existing data pertain to its efficacy and safety in the short to medium term due to the
relatively recent emergence of CXCR4 antagonists as treatment options. Thus, thorough long-term studies
are necessary to ensure that prolonged use of LY2510924 does not result in unforeseen complications or
adverse effects. These studies will play a crucial role in determining the longevity of LY2510924's
application in treating chronic conditions. Another challenge to consider is tailoring LY2510924 for
individual patient needs within the broader context of personalized medicine. The effectiveness of
LY2510924 may vary significantly depending on genetic factors, underlying conditions, and other
medications beyond simple pharmacokinetic and pharmacodynamic considerations. Developing assays or
biomarkers that predict patient responsiveness to LY2510924 could optimize its use, reduce
trial-and-error approaches, and enhance therapeutic outcomes, but such efforts are resource-intensive
and require substantial research and validation. Additionally, as with any new therapeutic compound,
regulatory hurdles can pose significant challenges in the development and application timeline.
LY2510924 will have to demonstrate stringent compliance with safety, efficacy, and ethical standards
imposed by healthcare regulatory bodies globally. This often involves an exhaustive approval process,
requiring convincing evidence from multiple well-documented and controlled trials, both in isolation and
in combination with existing therapies. However, despite these challenges, the future prospects for
LY2510924 are promising. Its role as a CXCR4 antagonist lends itself to a broad spectrum of potential
therapeutic applications, ranging from cancer to immune system disorders and possibly even in infectious
diseases such as HIV. As researchers deepen their understanding of LY2510924’s bioactivity and its
interaction in biological systems, new applications may come to light, catalyzing further advancements
in medical fields. Furthermore, in the context of evolving treatment paradigms, there is potential for
LY2510924 to be integrated into combination therapies where its CXCR4 inhibition complements other
therapeutic actions, potentially leading to synergistic outcomes that surpass current treatment
standards. Advances in drug delivery systems might enhance the bioavailability and targeted delivery of
LY2510924, maximizing its effectiveness while minimizing side effects. This aspect is especially
relevant given ongoing research into targeted therapies that offer precise, effective treatment with
minimal impact on healthy cells. Investing in these technologies will likely open new avenues for
reformulating LY2510924 into more patient-friendly and clinically-effective formats. Ultimately, while
there are challenges, the prospects for LY2510924 in treating multifaceted diseases through its distinct
mechanism of action suggest a bright future with potentially transformative impacts on patient care and
disease management.