1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR
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  3. SIBP-03

SIBP-03 is a specifical anti-HER3 antibody. SIBP-03 binds strongly and specifically to recombinant HER3 protein. SIBP-03 inhibits HER3 activation, as well as the downstream PI3K/AKT signaling pathway. SIBP-03 exhibits anticancer activity against squamous cell carcinoma, non-small cell lung cancer, gastric cancer, and breast cancer. SIBP-03 synergistically enhances the antitumor activity of DS-8201 (HY-138298A) and Cetuximab (HY-P9905).

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SIBP-03

SIBP-03 Chemical Structure

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Description

SIBP-03 is a specifical anti-HER3 antibody. SIBP-03 binds strongly and specifically to recombinant HER3 protein. SIBP-03 inhibits HER3 activation, as well as the downstream PI3K/AKT signaling pathway. SIBP-03 exhibits anticancer activity against squamous cell carcinoma, non-small cell lung cancer, gastric cancer, and breast cancer. SIBP-03 synergistically enhances the antitumor activity of DS-8201 (HY-138298A) and Cetuximab (HY-P9905)[1][2].

Isotype

Human IgG2 kappa

Recommend Isotype Controls
Species Reactivity

Human

IC50 & Target[1]

HER3

 

In Vitro

SIBP-03 (10-4-104 ng/mL) binds strongly and specifically to recombinant human HER3 protein, while no binding is detected with recombinant human EGFR, HER2 or HER4 proteins[1].
SIBP-03 binds to HER3 on the surface of MC38/HER3 cells with overexpressed HER3, while no detectable binding is observed with HER3-negative MC38 cells[1].
SIBP-03 (0.01-10 μg/mL; 24 h treatment of FaDu/BT-474 cells, with 2 h pre-incubation of cells stimulated by NRG1) effectively inhibits ligand-independent and ligand-dependent HER3 activation, as well as the downstream PI3K/AKT signaling pathway, in FaDu, BT-474, and NRG1-stimulated MCF7 and BT-474 cells[1].
SIBP-03 (0.01-100 μg/mL; 120 h) exerts only weak antiproliferative effects on FaDu, A549, BT-474, SK-BR-3 and NCI-N87 cells, but potently inhibits NRG1-stimulated proliferation of MCF7 cells, with an inhibition rate of 74.8% after treatment at 100 μg/mL[1].
SIBP-03 (10-100 μg/mL; 1 h) does not induce complement-dependent cytotoxicity in FaDu cells or HER3-overexpressing MC38/HER3 cells at concentrations of 10 and 100 μg/mL[1].
SIBP-03 (10-100 μg/mL; 5 h) induces ADCC activity in MC38/HER3 cells overexpressing HER3, but fails to induce such activity in BT-474 cells at concentrations of 10 and 100 μg/mL[1].
SIBP-03 (10-100 μg/mL; 5 h) induces antibody-dependent cellular phagocytosis activity in human breast cancer BT-474 cells and HER3-overexpressing MC38/HER3 cells at concentrations of 10 μg/mL and 100 μg/mL[1].
SIBP-03 (30 μg/mL; 144 h) can synergistically enhance the antiproliferative activity of DS-8201 in SK-BR-3 and MDA-MB-453 cells[2].

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

Cell Proliferation Assay[1]

Cell Line: Human head and neck squamous cell carcinoma FaDu cells, human non-small cell lung cancer A549 cells, human breast cancer BT-474 cells, human breast cancer SK-BR-3 cells, human gastric cancer NCI-N87 cells, NRG1-stimulated human breast cancer MCF7 cells
Concentration: 0.01-100 μg/mL
Incubation Time: 120 h
Result: Exhibited weak anti-proliferative effects, with inhibition rates ranging from 10.0% to 32.9% at 100 μg/mL in FaDu, A549, BT-474, SK-BR-3, and NCI-N87 cells.
Induced strong anti-proliferative effects, with 74.8% inhibition at 100 μg/mL in NRG1-stimulated MCF7 cells.
In Vivo

SIBP-03 (0.2-2 mg/kg; i.v.) exhibits potent antitumor activity in FaDu xenograft mouse models, with a TGI of 116.3% at the dose of 2 mg/kg, and produces sustained inhibition of the HER3/AKT signaling pathway for up to 168 h after a single intravenous administration[1].
SIBP-03 (6 mg/kg; i.v.) exhibits significant anti-tumor activity in the A549 xenograft mouse model, with a tumor growth inhibition (TGI) rate of 57.5% at the dose of 6 mg/kg[1].
SIBP-03 (20 mg/kg; i.v.) exhibits significant antitumor activity in the NCI-N87 xenograft mouse model, with a tumor growth inhibition (TGI) rate of 50.8% at the dose of 20 mg/kg[1].
Single treatment with SIBP-03 (0.6 mg/kg; i.v.) achieves a TGI of 96% in FaDu xenograft-bearing mice, while combination treatment with Cetuximab (HY-P9905) induces a TGI of 152% and causes tumor regression in 66.7% of treated mice[1].

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

Clinical Trial
Gene ID

2065  [NCBI]

Accession
Target

ERBB3/HER3

Application

ELISA, FACS, Functional assay

Conjugated

Unconjugated

Reconsititution

The product can be reconstituted/diluted with sterile PBS or saline.

SMILES

[SIBP-03]

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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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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SIBP-03
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HY-P991984
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