1. Immunology/Inflammation
  2. Interleukin Related
  3. MT204

MT204 is a humanized IgG1 antibody inhibitor targeting IL-2 of human and rhesus monkey origin. MT204 prevents soluble IL-2 from binding to intermediate-affinity IL-2 receptors and blocks CD25-bound IL-2 on high-affinity IL-2 receptors. MT204 has potently anti-proliferative activity with NKL cells and primary NK cells. MT204 has good tolerability and potent immunosuppressive activity in allogeneic skin graft model of rhesus monkey, promising for immunosuppressive and anti-proliferative therapy.

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MT204 Chemical Structure

MT204 Chemical Structure

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Description

MT204 is a humanized IgG1 antibody inhibitor targeting IL-2 of human and rhesus monkey origin. MT204 prevents soluble IL-2 from binding to intermediate-affinity IL-2 receptors and blocks CD25-bound IL-2 on high-affinity IL-2 receptors. MT204 has potently anti-proliferative activity with NKL cells and primary NK cells. MT204 has good tolerability and potent immunosuppressive activity in allogeneic skin graft model of rhesus monkey, promising for immunosuppressive and anti-proliferative therapy[1].

IC50 & Target

IL-2

0.58 nM (Kd)

In Vitro

MT204 (1-100 μg/mL, 4 days) dose-dependently inhibits proliferation and IFN-γ secretion in rhesus PBMCs stimulated by the mitogen concavalin A[1].
MT204 can block CD25-bound IL-2 on high-affinity IL-2 receptors with a kd of 0.58 nM[1][2].
MT204 (5 h) dose dependently reduces the IL-2 inducible cell surface expression of the alpha subunit of IL-4 receptor (CD124) in CTLL-2 cells[2].
MT204 (5 days) inhibits IL-2-induced proliferation of NKL cells and T cells with IC50 s of approximately 1.3 nM and 0.21 nM, respectively[2].
MT204 (15 min) potently antagonizes downstream signaling of IL-2 at sub-nanomolar concentrations, significantly reducing cellular pY-STAT3 levels stimulated by IL-2 in Primary human lymphocytes[2].
MT204 significantly inhibits IL-2 induced proliferation independently of CD25 expression levels in NKL cells, T cells and all NK cells with IC50 s of 0.35-0.36 nM, 0.33 nM, and 0.1-0.13 nM, respectively[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics
Species Dose Route Indicator value
Rhesus monkey 2, 10, 50 or repeat 50 mg/kg i.v. Cmax 1 mg/mL
Rhesus monkey 2, 10, 50 or repeat 50 mg/kg i.v. T1/2 326.4 hr
In Vivo

MT204 (50  mg/kg, i.v., day 0, day 5 and day 12 at a speed of 1.5 mL/kg/h over 1 h) significant delays in rejection of allogeneic skin graft in allogeneic skin graft model of rhesus monkey[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MHC-matched rhesus monkeys (Naive, captive bred, 3.8-9.6 k) were grafted on the inter-scapular area with circular MHC-mismatched rhesus skin (2 cm, lower abdomen)[1].
Dosage: 50 mg/kg
Administration: i.v., day 0, day 5 and day 12 at a speed of 1.5 ml/kg/h over 1 h, and then collected grafts and blood samples1.
Result: Extended graft survival to days 11, 13 and 14 (median day 13) compared vehicle-treatment (complete skin rejection on day 9.5).
Notably delayed necrosis of allogeneic grafts while the vehicle treated grafts showed complete necrosis since day 9.
Alleviated inflammation and inhibited multifocal epithelial hyperplasia with focal para-keratosis, and intra-epidermal infiltrates on epidermis. Potently antagonizes IL-2 in both CD25+ and CD25- cells.
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Storage

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MT204
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HY-P991270
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