1. Protein Tyrosine Kinase/RTK Antibody-Drug Conjugate/ADC Related
  2. c-Met/HGFR Radionuclide-Drug Conjugates (RDCs)
  3. DOTA-SMIC-1014

DOTA-SMIC-1014 is a DOTA chelator-conjugated precursor of the c-Met-targeting peptide SMIC-1014 (HY-P11863). DOTA-SMIC-1014 binds to the extracellular domain of c-Met (Kd = 42.83 nM). After radiolabeling to [68Ga]Ga-SMIC-1014, DOTA-SMIC-1014 acts as a positron emission tomography (PET) probe that achieves specific tumor uptake in xenografts and functions as a diagnostic probe targeting c-Met. SMIC-1014 can be used in research related to colon cancer, hepatocellular carcinoma, and prostate cancer.

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

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DOTA-SMIC-1014

DOTA-SMIC-1014 Chemical Structure

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Description

DOTA-SMIC-1014 is a DOTA chelator-conjugated precursor of the c-Met-targeting peptide SMIC-1014 (HY-P11863). DOTA-SMIC-1014 binds to the extracellular domain of c-Met (Kd = 42.83 nM). After radiolabeling to [68Ga]Ga-SMIC-1014, DOTA-SMIC-1014 acts as a positron emission tomography (PET) probe that achieves specific tumor uptake in xenografts and functions as a diagnostic probe targeting c-Met. SMIC-1014 can be used in research related to colon cancer, hepatocellular carcinoma, and prostate cancer[1].

In Vitro

[68Ga]Ga-SMIC-1014 binds to c-Met on HCT-116 human colon cancer cells, with a Kd value of 42.83 nM and a Bmax value of 188291 CPM, indicating high binding affinity[1].

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

In Vivo

DOTA-SMIC-1014 (800-fold molar excess; i.v.; single coinjection with [68Ga]Ga-SMIC-1014) significantly blocks specific c-Met-targeted tumor uptake of [68Ga]Ga-SMIC-1014 in HCT-116 xenografts mice, reducing uptake by ~66% at 30 minutes post-injection[1].

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

Animal Model: BALB/c nude (female, 8-10 weeks old, subcutaneous HCT-116 cell injection model)[1]
Dosage: 800-fold molar excess
Administration: i.v.; single coinjection with [68Ga]Ga-SMIC-1014
Result: Reduced tumor uptake of [68Ga]Ga-SMIC-1014 to 1.22 %ID/g at 30 min post-injection.
Reduced tumor uptake of [68Ga]Ga-SMIC-1014 to 0.93 %ID/g at 60 min post-injection.
Reduced tumor uptake of [68Ga]Ga-SMIC-1014 to 1.08 %ID/g in the 30-minute biodistribution study.
Decreased tumor uptake by ~66% at 30 minutes post-injection.
Molecular Weight

1571.69

Formula

C68H106N20O23

Sequence

DOTA-{βAla}-d{Arg-Leu-Asp}-Gly-d{Pro-Glu}-Gly-d{Pro-Phe-Gln}-NH2

Sequence Shortening

DOTA-{βAla}-d{RLD}-G-d{PE}-G-d{PFQ}-NH2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
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  • 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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Product Name:
DOTA-SMIC-1014
Cat. No.:
HY-P11864
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