DOTA-TH10
DOTA-TH10 is a CSPG4-targeted probe that enables targeted enrichment in tumors with overexpressed CSPG4. 68Ga-radiolabeled DOTA-TH10 specifically binds to CSPG4, allowing visualization of CSPG4 expression. 68Ga-radiolabeled DOTA-TH10 exhibits significant tumor uptake capacity in pancreatic cancer and gastric cancer models. DOTA-TH10 can be used for research on pancreatic cancer and gastric cancer.
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- Formule: C56H95N19O21S
- Masse moléculaire:1402.53
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Activité biologique
Description
In Vitro
DOTA-TH10 binds to purified CSPG4 protein with high affinity, with a docking score of −11.945[1].
DOTA-TH10 can be radiolabeled with 68Ga3+ with a labeling efficiency approaching 100%, forming [68Ga]Ga-DOTA-TH10 with a radiochemical purity of over 95%[1].
[68Ga]Ga-DOTA-TH10 (3 MBq; 120 min at 37 °C in PBS, pH 7.4) maintains strong in vitro stability for more than 120 min in PBS[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
[68Ga]Ga-DOTA-TH10 (5.5 MBq; intravenous injection; single dose) accumulates continuously in MKN45 gastric cancer xenografts within 90 min post-injection[1].
[68Ga]Ga-DOTA-TH10 (5.5 MBq; intravenous injection; single dose) shows extremely low uptake in HepG2 hepatocellular carcinoma xenografts (with low CSPG4 expression) at 60 min post-injection, with a tumor-to-muscle ratio of 2.00[1].
[68Ga]Ga-DOTA-TH10 (5.5 MBq; intravenous injection; single dose) has a circulating half-life of 20.75 min in healthy Balb/c mice, and exhibits favorable biosafety with no systemic toxicity detected within 15 days post-injection[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:T/B/NK triple immunodeficient (female)[1]
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Dosage:5.5 MBq; 5.5 MBq (coadministered with 2 mg unmodified TH10 peptide for blockade studies)
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Administration:i.v.; single injection
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Result:Reached tumor uptake of 2.07%ID/g at 30 min, 1.63%ID/g at 60 min, and 1.43%ID/g at 90 min in non-blocked ASPC1 tumor-bearing mice.
Showed tumor uptake of 0.88%ID/g at 60 min in blockade group, significantly lower than non-blocked group (P = 0.001881).
Achieved tumor-muscle ratios of 2.90 at 30 min, 3.62 at 60 min in non-blocked group, and 2.59 at 60 min in blockade group.
Demonstrated ASPC1 tumor uptake of 1.74%ID/g at 30 min, 1.38%ID/g at 60 min, and 0.85%ID/g at 90 min in biodistribution studies.
Showed 34.8% reduction in tumor uptake in 60 min blockade group (P = 0.019).
Exhibited lower uptake in healthy organs than tumor uptake, except for kidneys.
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Animal Model:T/B/NK triple immunodeficient (female)[1]
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Dosage:5.5 MBq
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Administration:i.v.; single injection
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Result:Exhibited persistent focal radioactivity accumulation at MKN45 tumor sites across 30, 60, and 90 min time points.
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Animal Model:T/B/NK triple immunodeficient (female)[1]
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Dosage:5.5 MBq
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Administration:i.v.; single injection
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Result:Reached tumor uptake of 0.60%ID/g at 60 min in HepG2 xenografts, significantly lower than uptake in ASPC1 xenografts (P = 0.000369).
Achieved tumor-muscle ratio of 2.00 at 60 min.
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Animal Model:Balb/c (female, healthy)[1]
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Dosage:5.5 MBq
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Administration:i.v.; single injection
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Result:Had a circulating half-life of 20.75 min.
Showed no statistically significant differences in serum biochemistry indicators (ALT, AST, ALP, BUN, CREA) or complete blood count parameters (RBC, WBC, PLT) between treated mice and controls.
Exhibited intact morphology of heart, liver, spleen, lungs, and kidneys with no inflammation, necrosis, or degenerative changes relative to controls in histological H&E staining at 15 days post-injection.
Chemical Information
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Masse moléculaire 1402.53
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Formule C56H95N19O21S
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Sequence
{DOTA}-Thr-Ala-Ala-Ser-Gly-Val-Arg-Ser-Met-His
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Sequence Shortening
{DOTA}-TAASGVRSMH
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DOTA-TH10 Related Classifications
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