44 Results for "

preclinical cell models

" in MedChemExpress (MCE) Product Catalog:
Products (44)

44 Results for "preclinical cell models" in MCE Product Catalog:

17
17 Publications Verification
Cat. No.: HY-13241A
CAS No.: 862505-00-8
Synonyms: LY2228820
Target:  

p38 MAPK Autophagy

Research Areas:  

Cancer

Ralimetinib is an ATP-competitive p38α and p38β MAPK inhibitor with an IC50 of 5.3 nmol/L against human p38α and an IC50 of 3.2 nmol/L against human p38β. Ralimetinib slows tumor growth in preclinical in vivo cancer models, exhibits oral bioavailability in mice, and achieves sustained target inhibition for 4 to 8 h. Ralimetinib is applicable for research on melanoma, non-small cell lung cancer, ovarian cancer, glioma, multiple myeloma, breast cancer, renal cancer, and head and neck squamous cell carcinoma .
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9
9 Cited Publications
Cat. No.: HY-100754
CAS No.: 1792180-81-4
Purity:  99.43%
Synonyms: PF-06651600
Research Areas:  

Inflammation/Immunology

Ritlecitinib (PF-06651600) is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC50=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC50 >10 μ M). Ritlecitinib rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE) .
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9
9 Cited Publications
Cat. No.: HY-100754C
CAS No.: 2192215-81-7
Purity:  99.77%
Synonyms: PF-06651600 tosylate
Research Areas:  

Inflammation/Immunology

Ritlecitinib (PF-06651600) tosylate is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC50=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC50 >10 μ M). Ritlecitinib tosylate rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib tosylate can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE) .
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7
7 Cited Publications
Cat. No.: HY-147214
CAS No.: 2648450-42-2
Purity:  99.54%
Target:  

YAP

Research Areas:  

Cancer

GNE-7883 is a pan-TEAD inhibitor that blocks the association of YAP/TAZ with TEAD. GNE-7883 effectively reduces chromatin accessibility at TEAD motifs, inhibits cell proliferation in multiple cell line models, and achieves strong anti-tumor efficacy in vivo. In addition, GNE-7883 effectively overcomes intrinsic and acquired resistance to KRAS (Kirsten rat sarcoma viral oncogene homolog) G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation .
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3
3 Cited Publications
Cat. No.: HY-164992
Synonyms: MRG002; Trastuzumab MMAE
Trastuzumab vedotin (MRG002; Trastuzumab MMAE) is an antibody-drug conjugate and cytotoxin targeting HER2, with a Kd of 7.50E-11 M for human HER2. After binding to HER2, Trastuzumab vedotin undergoes internalization and lysosomal trafficking, delivering a cytotoxic payload to HER2-expressing cells and inducing tumor regression in in vivo xenograft models with HER2-expressing tumors. The anti-tumor activity of Trastuzumab vedotin is enhanced when used in combination with anti-PD-1 antibodies, and it exhibits preclinical anti-tumor activity in drug-resistant breast cancer, gastric cancer, and urothelial carcinoma PDX models. Trastuzumab vedotin has low antibody-dependent cellular cytotoxicity activity and can be used in studies related to HER2-positive breast cancer, HER2-positive gastric cancer, and unresectable locally advanced or metastatic HER2-positive urothelial carcinoma .
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2
2 Cited Publications
Cat. No.: HY-P99463
CAS No.: 2268717-61-7
Synonyms: AVB-500; AVB-S6-500

Research Areas:  

Cancer

Batiraxcept (AVB-500; AVB-S6-500) is a selective, soluble AXL receptor and GAS6 inhibitor that targets the GAS6-AXL signaling axis. Batiraxcept is orally inactive and does not cross the blood-brain barrier. Batiraxcept competitively binds to GAS6 ((KD <1 nM), preventing its interaction with the AXL receptor tyrosine kinase, thereby inhibiting downstream PI3K/AKT and MAPK signaling pathways, reducing tumor cell glycolysis, angiogenesis, and metastatic potential. Batiraxcept has demonstrated antitumor activity in preclinical models of endometrial, cholangiocarcinoma, and ovarian cancer by inhibiting tumor growth, invasion, and metastasis .
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1
1 Cited Publications
Cat. No.: HY-119024
CAS No.: 112170-24-8
Purity:  98.88%
Target:  

SHP1 STAT

Research Areas:  

Cancer

BCI-137 is a Argonaute 2 (AGO2) inhibitor. By inhibiting AGO2 function, reducing PTPN6/SHP-1 protein levels and enhancing STAT1 phosphorylation, BCI-137 restores the sensitivity of tumor cells to IFN-γ. BCI-137 effectively enhances the recruitment, activation and cytotoxicity of CD8 + T cells. BCI-137 exerts a synergistic effect with anti-PD-1 antibodies and significantly reduces tumor volume in preclinical mouse models. BCI-137 exhibits favorable safety profiles and does not cause significant weight loss or death in mice. BCI-137 can be used in research related to bladder cancer, colorectal cancer, melanoma and other related fields .
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Cat. No.: HY-157941
CAS No.: 2267316-76-5
Purity:  99.89%
Synonyms: ART0380
Research Areas:  

Cancer

ART0380 is a potent, selective and orally active ATR kinase inhibitor. ART0380 potently inhibits human ATR-ATRIP complex with an IC50 of 51.7 nM. ART0380 binds the ATP pocket of the ATR-ATRIP complex, blocks ATR-dependent Chk1 serine 345 phosphorylation, and induces cell cycle disorder and DNA damage. ART0380 demonstrates potent and selective antitumor activity in preclinical models with varying types of ataxia-telangiectasia mutated (ATM) gene aberrancy. ART0380 can be used for the research of cancer, such as colorectal cancer and prostate cancer .
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Cat. No.: HY-P990673
Synonyms: DSTP-3086S Antibody; RG-7450 Antibody

Research Areas:  

Cancer

Vandortuzumab (DSTP-3086S Antibody; RG-7450 Antibody) is a humanized anti-STEAP1 IgG1 antibody and antimitotic agent that can be conjugated with MMAE (HY-15162) to form the antibody-drug conjugate (ADC) Vandortuzumab vedotin. Vandortuzumab vedotin specifically binds to STEAP1 and drives internalization of the complex, releasing the MMAE (HY-15162) payload intracellularly. After binding to tubulin, MMAE inhibits cell division and induces cell death. Vandortuzumab exhibits antitumor activity in preclinical xenograft models of prostate cancer and can be used for research related to metastatic castration-resistant prostate cancer (mCRPC) .
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Cat. No.: HY-163028
CAS No.: 459789-75-4
Target:  

Tim3

Research Areas:  

Cancer

ML-T7 is a potent Tim-3 inhibitor. ML-T7 blocks Tim-3 interactions with PtdSer and CEACAM1. ML-T7 not only enhances the antitumor activity of adoptive transfer therapy with cytotoxic T lymphocytes (CTLs) and CAR T cells but also increases the effector function of T cell. ML-T7 promotes NK cells’ killing activity against tumor cells and DC antigen-presenting capacity. ML-T7 directly exerts antitumor efficacy in preclinical tumor models either alone or in combination with Nivolumab (HY-P9903A). ML-T7 can be used for tumor immunotherapy research .
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Cat. No.: HY-P990083
CAS No.: 2628092-47-5
Synonyms: AT-1501

Target:  

TNF Receptor

Research Areas:  

Inflammation/Immunology

Tegoprubart (AT-1501) is a CD40 ligand inhibitor (EC50=100 ng/mL) and immunosuppressant that selectively inhibits the CD40 ligand, a co-stimulatory molecule involved in T cell activation. Tegoprubart suppresses immune rejection, prevents rejection in animal transplantation models, and reduces cell-mediated and antibody-mediated immune responses to create a more immunotolerant environment. Tegoprubart preserves renal function when combined with Mycophenolate (HY-B0421) and Corticosteroids, and maintains graft function in preclinical studies. Tegoprubart is applicable to research related to kidney transplantation and kidney transplant rejection .
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Cat. No.: HY-173178
CAS No.: 925419-55-2
Research Areas:  

Cancer

LNS8801 is an orally active GPER activator with tumor suppressor activity. LNS8801 mediates suppression of cancer via GPER activation, with activity dependent on GPER expression. LNS8801 suppresses cancer growth in preclinical models. LNS8801 can be used for the research of cancer (including melanoma, pancreatic ductal adenocarcinoma, non-small cell lung cancer, leukemias, colon carcinomas) .
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Cat. No.: HY-P1615
CAS No.: 1006388-38-0
Synonyms: UPARANT
Cenupatide (UPARANT) is a uPAR and FPR antagonist with anti-angiogenic, anti-inflammatory, and vascular barrier regulatory activities, as well as high stability and resistance to enzymatic degradation in blood/plasma. Cenupatide blocks the uPAR-FPR interaction, reduces VEGF-induced phosphorylation levels of AKT, VEGFR-2, STAT3, JNK, p38 MAPK, ERK1/2, and NF-κB p65, and inhibits αvβ3 integrin activation. Cenupatide suppresses endothelial cell migration, invasion, tube formation, and angiogenic signaling pathways, restores tight junctions and blood-retinal barrier integrity, reduces pro-inflammatory marker levels, and inhibits apoptosis. Cenupatide reduces retinal neovascularization, renal fibrosis, and vascular leakage, and restores visual function in preclinical models. Cenupatide is applicable to research related to retinopathy, diabetic complications, ocular diseases, cancer, and inflammatory diseases .
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Cat. No.: HY-145996
CAS No.: 401513-39-1
Target:  

Others

Research Areas:  

Cardiovascular Disease Infection

STC314 is a histone-neutralizing agent. STC314 inhibits histone-mediated cytotoxicity, blocks histone-induced erythrocyte aggregation, reduces fragility, restores deformability and inhibits histone-induced aggregation and degranulation in human erythrocytes. STC314 reduces histone-mediated tissue damage, thrombocytopenia, anemia, and cell death, and improves survival in preclinical models. STC314 can be used for the research of sepsis, ischemia-reperfusion injury, and deep-vein thrombosis .
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Cat. No.: HY-164725
CAS No.: 3023869-94-2
Research Areas:  

Cancer

FAPI-mFS is a selective fibroblast activation protein (FAP) inhibitor with an IC50 of 0.0014 μM against human FAP. Through its covalent binding property with FAP, FAPI-mFS enhances its uptake and retention time in cancer cells. When radiolabeled with 68Ga, FAPI-mFS serves as a PET/CT imaging agent with superior tumor-to-background tissue contrast and lesion detection capability. When radiolabeled with 177Lu or 225Ac, FAPI-mFS induces tumor regression and inhibition in preclinical models. FAPI-mFS can be used in studies related to cancer and radionuclide-conjugated drugs (RDC) .
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Cat. No.: HY-100754A
CAS No.: 2140301-97-7
Synonyms: PF-06651600 malonate
Research Areas:  

Inflammation/Immunology

Ritlecitinib (PF-06651600) malonate is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC50=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC50 >10 μ M). Ritlecitinib malonate rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib malonate can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE) .
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Cat. No.: HY-158046
CAS No.: 3094059-37-4
Target:  

PROTACs STING

Research Areas:  

Cancer

UNC8899 is a STING PROTAC degrader with a DC50 of 1.097 μM. UNC8899 recruits the VHL E3 ligase to mediate the ubiquitination of phosphorylated STING and subsequent proteasomal degradation. UNC8899 can be used in studies of renal cell carcinoma .
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Cat. No.: HY-W224634
CAS No.: 304453-52-9
Target:  

HSP

Research Areas:  

Cancer

HSF1-IN-2 (Compound 0048) is a HSF1 inhibitor. HSF1-IN-2 is applicable to cancer research .
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Cat. No.: HY-114584
CAS No.: 1037826-77-9
Target:  

Ser/Thr Protease

Research Areas:  

Neurological Disease

A-953227 is a highly potent and selective inhibitor with the activity of inhibiting calcium-dependent esterase (calpain). A-953227 has enhanced selectivity for related cysteine proteases (cathepsins) and has shown good efficacy in cell experiments. A-953227 has shown broad efficacy in preclinical models for Alzheimer's disease, suggesting that it has potential benefits in inhibiting Alzheimer's disease .
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Cat. No.: HY-186087
CAS No.: 3058972-05-4
Target:  

Ras ERK Cyclophilin

Research Areas:  

Cancer

RM-046 is an orally active, selective ternary complex inhibitor of KRAS Q61H (active form). RM-046 forms a ternary complex with cyclophilin A, binds to active KRAS Q61H in a non-covalent manner, blocks effector binding via steric hindrance and inhibits downstream signal transduction. RM-046 inhibits ERK phosphorylation and cancer cell proliferation, and induces sustained RAS pathway signal inhibition, anti-tumor activity and tumor regression in preclinical xenograft models. RM-046 can be used for the research of KRAS Q61H mutant cancers .
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