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.
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Biological Activity
Human
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.
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Cell Line:HER2-positive human breast cancer BT-474, SK-BR-3, AU-565 cells; NCI-N87 cells
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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)
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Incubation Time:6 days (BT-474); 3 or 6 days (SK-BR-3, AU-565, NCI-N87)
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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.
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Cell Line:HER2-positive human breast cancer BT-474 cells
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Concentration:100 nM
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Incubation Time:72 h
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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.
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Cell Line:HER2-positive human breast cancer BT-474 cells
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Concentration:10 μg/mL
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Incubation Time:3 days
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Result:Induced significantly increased cleavage of PARP, a marker of apoptosis combinated with Trastuzumab.
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Cell Line:HER2-positive human breast cancer BT-474 cells
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Concentration:100 nM
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Incubation Time:3 days
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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.
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.
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Animal Model:NOD SCID (6 to 8-week-old; subcutaneous inoculation of NCI-N87 cells)[1]
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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)
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Administration:i.p.; twice weekly
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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.
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Animal Model:NOD SCID (6 to 8-week-old; subcutaneous inoculation of BT-474 cells)[1]
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Dosage:3 mg/kg + 3 mg/kg Trastuzumab
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Administration:i.p.; twice weekly
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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.
ERBB2/HER2/CD340
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Product Image
ELISA, FACS, Functional assay
Chemical Information
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SMILES
[BSI-001]
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Synonyms
5G9
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BSI-001 Related Classifications
HY-P991977 Related Classifications
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