amg-1

AMG-1 is a specific CRAC channel inhibitor. AMG-1 blocks the function of effector T cells, but not regulatory T cells in vitro and it attenuates the progression and severity of EAE in vivo.

AMG-Tie2-1 is a dual inhibitor of VEGF receptor 2 (VEGFR2) and tunica interna endothelial cell kinase 2 (Tie2).

AMG-25 (c-Kit-IN-5-1) is a selective and potent c-Kit inhibitor that inhibits c-Kit, KDR, p38, Lck, and Src, and can be used in the study of mast cell-associated fibrosis.

SYN1143 (AMG-1) is a potent inhibitor of human RON and c-Met.In vitro kinase assays showed that compound I is a potent inhibitor of human RON and c-Met with IC50s of 9 and 4 nmol/L, respectively.

AMG-0347 (UNII-CD7L9290QR) is a small molecule inhibitor targeting TRPA1(transient receptor potential ankyrin 1) ion channels, a receptor found in sensory neurons and involved in the detection of pain and environmental stimuli. AMG-0347 acts by blocking the function of TRPA1 and has analgesic effects.

AMG-1694, a potent disruptor of the glucokinase–glucokinase regulatory protein (GK-GKRP) complex, operates by promoting the dissociation of this complex, thereby indirectly enhancing GK enzymatic activity with an IC50 of 7 nM. It effectively normalizes blood glucose levels in various rodent diabetes models [1] and lowers blood glucose specifically in diabetic animals without affecting normoglycemic ones. Additionally, AMG-1694 reverses the GKRP-induced inhibition of GK activity and facilitates GK translocation.

AMG 517 is an effective and specific TRPV1 antagonist, antagonizes proton (IC50: 0.76 nM), capsaicin (IC50: 0.62 nM), and heat activation (IC50: 1.3 nM) of TRPV1.

Tarlatamab (AMG-757) is a first-in-class, high-affinity, bispecific T-cell engager (BiTE) antibody that selectively targets delta-like ligand 3 (DLL3), a protein predominantly expressed in small-cell lung cancer (SCLC) tumors with minimal expression in normal tissues. It demonstrates dissociation constants (KDs) of 0.64 nM and 0.50 nM for DLL3 in human and nonhuman primates (NHP), respectively, and 14.9 nM and 12 nM for CD3 in human and NHP, accordingly. As a pioneering HLE BiTE immuno-oncology therapy for DLL3-expression SCLC, tarlatamab shows promising potential for research in this area [1].

Rocatinlimab (AMG 451) (KHK4083) is a fully human, non-fucosylated IgG1 anti-OX40 monoclonal antibody indicated for atopic dermatitis (AD) research [1].

Gresonitamab (AMG 910), a half-life extended (HLE) bispecific T-cell engager (BiTE) antibody, specifically targets CD3-positive T cells and CLDN18.2-expressing tumor cells, offering potential research applications in adenocarcinoma [1].

Solitomab (AMG 110), a bispecific antibody targeting CD3 and EpCAM, is utilized in researching primary uterine and ovarian carcinosarcoma cancer [1] [2].

Pacanalotamab (AMG 420; BI-836909) is a bispecific T-cell engager (BiTE) that specifically targets BCMA (B cell maturation antigen) and CD3ɛ. By redirecting T cells to cells expressing BCMA on their surface, Pacanalotamab facilitates the T-cell mediated lysis of human multiple myeloma (MM) cell lines [1].

Brazikumab (AMG 139), a human IgG2 monoclonal antibody, selectively targets the p19 subunit of IL-23 with a dissociation constant (K D) of 0.138 nM, indicating high affinity for human IL-23. It is employed in Crohn's disease research [1].

AMG-208 is a highly selective c-Met inhibitor with IC50 of 9 nM. Phase 1.

Vepsitamab (AMG 199) is an anti-MUC17/CD3 BiTE antibody that engages both CD3 on T cells and MUC17 on tumor cells, facilitating targeted tumor cell destruction while stimulating T cell activation and proliferation [1].

Pavurutamab (AMG-701) is a bispecific T-cell engager that targets CD3 and B-cell maturation antigens (BCMA), based on the extended half-life derived from Pacanalotamab. Its Fc region is engineered for improved pharmacokinetics, offering potential in immune regulation and the treatment of multiple myeloma (MM) [1] [2] [3] [4].

AMG-176 is a MCL-1 inhibitor (Ki: 0.13 nM).

AMG 925 is a potent and orally bioavailable dual FLT3/CDK4 inhibitor with IC50 of 1 nM and 3 nM, respectively.

AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents. IC50 value: 13 nM (EC50) [1] Target: GPR40 agonist AMG 837 displayed the expected t

AMG 837 is a partial GPR40 agonist with an EC50 value of 13 nM, showcasing 85% of the maximal activity displayed by DHA in standard assay conditions, indicating its high potency and selectivity in vitro. This compound excels as a GPR40 agonist with a notable pharmacokinetic profile, effectively stimulating insulin secretion in a glucose-dependent manner in rodents and demonstrating potent insulin secretion stimulation in MIN6 cells, with efficacy comparable to that observed in aequorin Ca2+-flux assays. Moreover, AMG 837 exhibits a two-fold increase in potency compared to its racemic counterpart on GPR40, with demonstrated activity across rat and mouse GPR40 versions (EC50 = 23 and 13 nM, respectively). It lacks significant activity against PPARα, δ, and γ in cell-based assays, and an analysis against an external panel of 64 receptors revealed negligible activity, except for a weak inhibition (IC50 = 3 μM) on the a2-adrenergic receptor.

AMG 925 HCl is a selective and potent dual inhibitor of FLT3 (IC50: 2±1 nM) and CDK4 (IC50: 3±1 nM).

AMG-315 is a Potent Endocannabinoid Ligand with Stability to Metabolizing Enzymes. AMG-315 is a chiral arachidonoyl ethanolamide (AEA) analogue or (13S,1′R)-dimethylanandamide. AMG-315 is a high affinity ligand for the CB1 receptor (Ki of 7.8 ± 1.4 nM) that behaves as a potent CB1 agonist in vitro (EC50 = 0.6 ± 0.2 nM). AMG-315 is the first potent AEA analogue with significant stability for all endocannabinoid hydrolyzing enzymes as well as the oxidative enzymes COX-2. AMG-315 will serve as a very useful endocannabinoid probe.

Zelminemab (AMG-301) is a human monoclonal antibody designed to target and inhibit the PACAP type I (PAC1) receptor [1].

BI-0314 is a selective allosteric STEP activator.

AMG-548 dihydrochloride is a selective, orally active p38α inhibitor with a Ki value of 0.5 nM, a slight selectivity for p38β (Ki=36 nM) and >1000-fold selectivity for p38γ and p38δ. AMG-548 dihydrochloride exhibits inhibition of whole blood LPS-stimulated TNFα with an IC50 value of 3 nM. AMG-548 dihydrochloride directly inhibited casein kinase 1 isoforms δ and ε, and inhibited Wnt signaling.

AMG-548 hydrochloride is a selective, orally active p38α inhibitor with a Ki value of 0.5 nM, a slight selectivity for p38β (Ki=36 nM) and a 1000-fold selectivity for p38γ and p38δ. AMG 548 hydrochloride also effectively inhibits whole blood LPS-stimulated TNFα with an IC50 value of 3 nM. AMG-548 hydrochloride directly inhibited casein kinase 1 isoforms δ and ε, which in turn inhibited Wnt signaling.

AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks(Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively). It exhibits anti-tumor activity in mouse glioblastoma xenograft model[1]. AMG 511 significantly suppresses PI3K

AMG-47a is a potent inhibitor of Lck and T cell proliferation. AMG-47a could promote the degradation of the KRAS oncoprotein. AMG-47a selectively reduced the levels of EGFP-KRASG12V protein but did not affect EGFP protein in cells.

Zeluvalimab (AMG-404) is a monoclonal antibody designed to target the PD-1 receptor, and is utilized in cancer research [1].

Latikafusp (AMG 256), a bifunctional fusion protein, combines a PD-1-targeting antibody with an IL-21 mutein, facilitating IL-21 pathway stimulation in PD-1+ cells. It aims to enhance and sustain the functionality of cytotoxic and memory T cells, thereby inducing anti-tumor immunity. This compound shows promise for research in solid tumors [1] [2].

Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity (IC50: 5.9 nM).

Ganitumab (AMG 479) is a highly potent monoclonal antibody to type 1 insulin-like growth factor receptor (IGF1R). Ganitumab is recognized to bind to IGF1R at low concentration with KD value of 0.22 nM. Ganitumab can inhibit the interaction of IGF1R with IGF1 and IGF2 in mice. Ganitumab can be used to study cancer.

AMG-548 is an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ and is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM

AMG 9810 is a competitive antagonist of capsaicin activation of the vanilloid receptor 1 (TRPV1) (IC50s = 24.5 and 85.6 nM for human and rat TRPV1, respectively).

AMG-076 is an antagonist of melanin-concentrating hormone receptor 1. It also reduced hERG inhibition.

AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A/B/C with IC50 of 5 nM/4 nM /1 nM. It is >10-fold selective for Aurora kinases than p38α, Tyk2, JNK2, Met and Tie2. Phase 1.

Conatumumab (AMG 655) is a monoclonal agonist antibody targeting human death receptor 5 (DR5, TRAILR2) at Kd 1 nM for long DR5 and Kd 0.8 nM for short DR5. Conatumumab induces apoptosis in a variety of tumor types through caspase activation. Conatumumab can be used to study advanced solid tumors.