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humanized mouse model

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By Targets:	CCR (1) Complement System (1) Dihydroorotate Dehydrogenase (1) HIV (1) Interleukin Related (1) Microtubule/Tubulin (1) Parasite (3) PD-1/PD-L1 (3) TNF Receptor (1)
By Research Areas:	Cancer (8) Infection (4) Inflammation/Immunology (2)

11

Inhibitors & Agonists

5

Inhibitory Antibodies

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

Cys-McMMAF	Microtubule/Tubulin	Cancer
Cys-McMMAF is the released payload of AlMcMMAF, an anti-5T4 humanized A1 antibody conjugated to the microtubule disrupting MMAF (HY-15579) via a maleimidocaproyl linker. Cys-McMMAF has antitumor efficacy in two tumor mouse models (H1975 and MDA-MB-361-DYT2 models) .

Leronlimab PRO 140	CCR HIV	Infection Cancer
Leronlimab (PRO 140) is a humanized IgG4 anti-CCR5 monoclonal antibody. Leronlimab inhibits CCR5-mediated HIV-1 viral and lung metastasis in mouse tumor models. Leronlimab can be used for the research of HIV nonalcoholic steatohepatitis (NASH) and cancer .

ARB-272572	PD-1/PD-L1	Cancer
ARB-272572 is an oral effective small molecule PD-L1 inhibitor, with an IC₅₀ value of 400 pM. ARB-272572 has research significance in tumors and chronic viral infections .

MMV688533	Parasite	Infection
MMV688533 is an antimalarial agent with rapid anti-plasmodial activity and effective single-dose activity against Plasmodium falciparum infection in humanized mouse models. MMV688533 can inhibit the activity of asexual blood stage parasites with an IC₅₀ value of 1.3 nM. MMV688533 exhibits excellent pharmacokinetic properties and safety .

Empasiprubart ARGX-117	Complement System	Inflammation/Immunology
Empasiprubar (ARGX-117) is a humanized inhibitory monoclonal antibody targeting complement C2. Empasiprubar binds to the Sushi-2 domain of C2, preventing the formation of C3 pre convertase and inhibiting the activation of classical and lectin pathways upstream of C3 activation. Empasiprubar can prevent complement mediated autoimmune hemolytic anemia and antibody mediated organ transplant rejection. Empasiprubar can prevent neuroglial lymphoconjunctival injury in GM1 antibody mediated mouse models .

Utomilumab PF 05082566	TNF Receptor	Inflammation/Immunology Cancer
Utomilumab (PF 05082566) is a fully human IgG2 agonist monoclonal antibody that selectively binds to 4-1BB/CD137. Utomilumab can be used in the research of tumors such as follicular and other CD20 ⁺ non-Hodgkin lymphomas .

PD-1/PD-L1-IN-48	PD-1/PD-L1	Cancer
PD-1/PD-L1-IN-48 (compound HD10) is a potent inhibitor of PD-1/PD-L1 interaction, with an IC₅₀ of 3.1 nM. PD-1/PD-L1-IN-48 plays an important role in cancer research .

DSM1465	Parasite Dihydroorotate Dehydrogenase	Infection
DSM1465 (Compound 82) is a potent, selective inhibitor of P. falciparum dihydroorotate dehydrogenase (PfDHODH) with an IC₅₀ value of 15 nM, inhibits P. falciparum 3D7 (Pf3D7) parasites with an EC₅₀ value of 1.4 nM. DSM1465 shows potent in vivo activity in the humanized P. falciparum mouse model .

PD-1/PD-L1-IN-32	PD-1/PD-L1	Cancer
PD-1/PD-L1-IN-32 (compound A56) is a potent PD-1/PD-L1 inhibitor (IC₅₀=2.4 nM), with anticancer activity. PD-1/PD-L1-IN-32 significantly inhibits tumor growth in hPD-L1 MC38 humanized mouse model, without obvious toxicity against mouse normal ability .

(Rac)-ACT-451840	Parasite	Infection
(Rac)-ACT-451840 is an isomer of ACT-451840 that exhibits significant antimalarial effects. (Rac)-ACT-451840 exhibits significant antimalarial activity against P. berghei-infected mice at a dose of 20 mg/kg (ED90=13 mg/kg), and has an inhibitory effect at a dose of 300 mg/kg. The ED90 of (Rac)-ACT-451840 in the P. falciparum humanized immunodeficient mouse model is 3.7 mg/kg. (Rac)-ACT-451840 is similar to artemisinin, with a rapid onset of action but requires repeated high doses.

Talacotuzumab JNJ 56022473; CSL 362	Interleukin Related	Cancer
Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has K_Ds of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .

Cat. No.	Product Name	Target	Research Area

Leronlimab PRO 140	CCR HIV	Infection Cancer
Leronlimab (PRO 140) is a humanized IgG4 anti-CCR5 monoclonal antibody. Leronlimab inhibits CCR5-mediated HIV-1 viral and lung metastasis in mouse tumor models. Leronlimab can be used for the research of HIV nonalcoholic steatohepatitis (NASH) and cancer .

Empasiprubart ARGX-117	Complement System	Inflammation/Immunology
Empasiprubar (ARGX-117) is a humanized inhibitory monoclonal antibody targeting complement C2. Empasiprubar binds to the Sushi-2 domain of C2, preventing the formation of C3 pre convertase and inhibiting the activation of classical and lectin pathways upstream of C3 activation. Empasiprubar can prevent complement mediated autoimmune hemolytic anemia and antibody mediated organ transplant rejection. Empasiprubar can prevent neuroglial lymphoconjunctival injury in GM1 antibody mediated mouse models .

Utomilumab PF 05082566	TNF Receptor	Inflammation/Immunology Cancer
Utomilumab (PF 05082566) is a fully human IgG2 agonist monoclonal antibody that selectively binds to 4-1BB/CD137. Utomilumab can be used in the research of tumors such as follicular and other CD20 ⁺ non-Hodgkin lymphomas .

Talacotuzumab JNJ 56022473; CSL 362	Interleukin Related	Cancer
Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has K_Ds of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .

MK-4830	Inhibitory Antibodies	Cancer
MK-4830 is a fully humanized monoclonal antibody of the immunoglobulin G4 subclass that specifically binds to ILT4 and blocks its interaction with HLA-G and other ligands. MK-4830 inhibits tumor growth in humanized mouse cancer models .

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