2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis Cell Cycle/DNA Damage Epigenetics PI3K/Akt/mTOR MAPK/ERK Pathway Stem Cell/Wnt
  3. EGFR Apoptosis PARP Akt ERK
  4. BSI-001

BSI-001 (5G9) is a HER2-targeting antibody. BSI-001 inhibits cell proliferation and migration, induces apoptosis and PARP cleavage, and suppresses HER2-mediated downstream signaling pathways (including the phosphorylation of EGFR, HER3, AKT and ERK) when combined with Trastuzumab (HY-P9907) in HER2-positive cancer cells. BSI-001 exhibits synergistic anti-tumor efficacy in animal models of gastric cancer and breast cancer when combined with Trastuzumab. BSI-001 can be used for the research of HER2-positive breast cancer and HER2-overexpressing gastric cancer.

For research use only. We do not sell to patients.

BSI-001

BSI-001 Chemical Structure

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BSI-001 Related Antibodies

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Description

BSI-001 (5G9) is a HER2-targeting antibody. BSI-001 inhibits cell proliferation and migration, induces apoptosis and PARP cleavage, and suppresses HER2-mediated downstream signaling pathways (including the phosphorylation of EGFR, HER3, AKT and ERK) when combined with Trastuzumab (HY-P9907) in HER2-positive cancer cells. BSI-001 exhibits synergistic anti-tumor efficacy in animal models of gastric cancer and breast cancer when combined with Trastuzumab. BSI-001 can be used for the research of HER2-positive breast cancer and HER2-overexpressing gastric cancer[1].

Species Reactivity

Human
In Vitro

BSI-001 binds strongly to BT-474 and SK-BR-3 cells with overexpressed HER2[1].
BSI-001 (100 nM, serially diluted; 3-6 days) exerts weak inhibitory effects on the proliferation of HER2-positive cancer cells when used alone, but it exerts potent synergistic anti-proliferative effects in multiple HER2-positive cancer cell lines when combined with Trastuzumab (HY-P9907) at a fixed dose ratio of 1:1[1].
BSI-001 (72 h) potently inhibits the migration of BT-474 cells when combined with Trastuzumab[1].
BSI-001 (100 nM; 72 h) = induces late-stage apoptosis and PARP cleavage in BT-474 cells when combined with Trastuzumab[1].
BSI-001 (100 nM; 3 days) reduces the total HER2 protein level in BT-474 cells and inhibits HER2-mediated downstream signaling pathways (including the phosphorylation of EGFR, HER3, AKT and ERK) when combined with Trastuzumab[1].

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

BSI-001 Related Antibodies

Cell Viability Assay[1]

Cell Line: HER2-positive human breast cancer BT-474, SK-BR-3, AU-565 cells; NCI-N87 cells
Concentration: 100 nM (single agent for SK-BR-3, AU-565, NCI-N87); serially diluted (alone or 1:1 fixed-dose ratio with trastuzumab for BT-474)
Incubation Time: 6 days (BT-474); 3 or 6 days (SK-BR-3, AU-565, NCI-N87)
Result: Alone exhibited weak inhibition of BT-474 cell proliferation.
In combination with Trastuzumab, showed substantially enhanced BT-474 cell proliferation inhibition compared to single agents.
Showed stronger synergism between 5G9 and trastuzumab.
In SK-BR-3, AU-565, and NCI-N87 cells, the combination of 5G9 and trastuzumab reduced cell viability more effectively.

Apoptosis Analysis[1]

Cell Line: HER2-positive human breast cancer BT-474 cells
Concentration: 100 nM
Incubation Time: 72 h
Result: Resulted in a significantly lower number of viable BT-474 cells and a higher level of late-stage apoptosis combinated with Trastuzumab, compared to the trastuzumab-pertuzumab combination.

Western Blot Analysis[1]

Cell Line: HER2-positive human breast cancer BT-474 cells
Concentration: 10 μg/mL
Incubation Time: 3 days
Result: Induced significantly increased cleavage of PARP, a marker of apoptosis combinated with Trastuzumab.

Western Blot Analysis[1]

Cell Line: HER2-positive human breast cancer BT-474 cells
Concentration: 100 nM
Incubation Time: 3 days
Result: Reduced total and phosphorylated HER2 protein levels, and also reduced phosphorylated levels of EGFR, HER3, AKT, and ERK (total protein levels of these targets remained unchanged) combinated with Trastuzumab.
In Vivo

BSI-001 (5-15 mg/kg; i.p.; twice weekly) exerts potent synergistic anti-tumor activity in the NCI-N87 gastric cancer xenograft model when combined with Trastuzumab[1].
BSI-001(3 mg/kg; i.p.; twice weekly) exerts potent synergistic anti-tumor activity in combination with Trastuzumab in the BT-474 breast cancer xenograft model[1].

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

Animal Model: NOD SCID (6 to 8-week-old; subcutaneous inoculation of NCI-N87 cells)[1]
Dosage: 5 mg/kg (monotherapy, TGI); 5 mg/kg + 5 mg/kg Trastuzumab (combination, TGI); 15 mg/kg + 15 mg/kg Trastuzumab (combination, tumor eradication)
Administration: i.p.; twice weekly
Result: Resulted in a tumor growth inhibition (TGI) of 18.16%.
Achieved a TGI of 98.31%, with a day 22 mean tumor volume of 8.75 mm3, which was significantly higher than 15 mg/kg Trastuzumab monotherapy.
Eradicated tumors in 6 out of 7 mice, with no significant tumor regrowth observed through day 63, whereas Trastuzumab plus pertuzumab at the same dose showed tumor progression.
Showed a significantly higher TGI than the Trastuzumab plus pertuzumab combination at the same dose.
Animal Model: NOD SCID (6 to 8-week-old; subcutaneous inoculation of BT-474 cells)[1]
Dosage: 3 mg/kg + 3 mg/kg Trastuzumab
Administration: i.p.; twice weekly
Result: Resulted in a TGI of 47%, which was significantly higher than the 24% TGI achieved by the same-dose combination of Trastuzumab plus pertuzumab.
Reduced final mean tumor mass significantly compared to the pertuzumab combination group.
Gene ID

2064  [NCBI]

Accession
Target

ERBB2/HER2/CD340
Application

ELISA, FACS, Functional assay
Conjugated

Unconjugated
Reconsititution

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

[BSI-001]
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BSI-001 Related Classifications

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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.

Keywords:

BSI-0015G9BSI001BSI 001EGFRApoptosisPARPAktERKEpidermal growth factor receptorErbB-1HER1poly ADP ribose polymerase PKBProtein kinase BExtracellular signal regulated kinasesHER2-targeting antibodyBT-474 cellsSK-BR-3 cellsbreast cancergastric cancer
Inhibitorinhibitorinhibit

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