P-LPK
P-LPK is a dodecapeptide that specifically targets SLC1A5, which is highly expressed on the membrane of colorectal cancer cells, with a Kd value of 1.19 μM. P-LPK has no intrinsic cell proliferation regulatory activity. Gallium-68-labeled P-LPK selectively accumulates at colorectal cancer tumor sites in xenograft mouse models. P-LPK can serve as a targeted carrier to deliver Camptothecin (HY-16560) to colorectal cancer cells, forming the conjugate P-LPK-CPT. P-LPK can be used in the research of colorectal cancer.
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- Fòrmula: C54H94N14O20S
- Peso molecular:1291.47
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Almacenamiento:
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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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
P-LPK (2 h) binds selectively to the cell membranes of human colorectal cancer cell lines Colo320HSR, HCT116 and LoVo, and its binding capacity is significantly higher than that of untransformed human colonic epithelial cells NCM460[1].
P-LPK binds selectively to human colorectal cancer (CRC) tissues, and its binding capacity is significantly higher than that to adjacent normal human colonic tissues[1].
P-LPK (overnight) colocalizes with SLC1A5 on the cell membrane of human colorectal cancer HCT116 cells, while mutations in P-LPK disrupt this interaction[1].
P-LPK (24-72 h) exhibits no cytotoxicity or proliferation-regulating effects on human colorectal cancer HCT116 cells, LoVo cells, and untransformed human colonic epithelial NCM460 cells[1].
P-LPK is mainly internalized into human colorectal cancer HCT116 cells via a clathrin-mediated endocytosis mechanism[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 4 weeks old)[1]
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Dosage:3.7 MBq (100 μCi, 0.1 nmol in 100 μl) (68Ga-P-LPK); unlabeled P-LPK (blocking experiment)
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Administration:i.v.; single dose; pre-injection (blocking experiment)
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Result:Showed remarkable accumulation in HCT116 tumors at all time points, with significantly higher tumor/non-tumor (T/NT) ratios compared to 68Ga-P-CON.
Demonstrated no significant accumulation in U87 tumors.
Dramatically attenuated 68Ga-P-LPK binding to HCT116 tumors when pre-injected as unlabeled P-LPK, significantly reducing T/NT ratios at 60 and 120 minutes.
Chemical Information
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Peso molecular 1291.47
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Fòrmula C54H94N14O20S
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Sequence
Leu-Pro-Lys-Thr-Val-Ser-Ser-Asp-Met-Ser-Leu-Asn
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Sequence Shortening
LPKTVSSDMSLN
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
P-LPK Related Classifications
HY-P11756 Related Classifications
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