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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- References
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Biological Activity
Description
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.
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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.
In Vivo
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.
Gene ID
Accession
Target
ERBB2/HER2/CD340
Conjugated
Unconjugated
Reconsititution
The product can be reconstituted/diluted with sterile PBS or saline.
Format
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Product Image
Application
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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