Raludotatug Deruxtecan
Based on 1 Customer Validation
Raludotatug Deruxtecan is an antibody-drug conjugate targeting CDH6, with an EC50 of 64.7 ng/mL in humans, 70.4 ng/mL in cynomolgus monkeys, and 228 ng/mL in mice. Raludotatug Deruxtecan specifically binds to CDH6 on the surface of cancer cells, triggers lysosomal internalization, and releases the DXd payload that inhibits TOP1. Raludotatug Deruxtecan induces DNA damage, Chk1 phosphorylation, caspase-3 cleavage, apoptosis, and bystander cell death. Raludotatug Deruxtecan is applicable to research related to serous ovarian cancer and renal cell carcinoma.
For research use only. We do not sell to patients.
- Purity: 98.68%
- CAS No.: 2610074-57-0
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Storage:
-80°C, protect from light
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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Raludotatug deruxtecan (R-DXd) (0.001-1000 ng/mL; 6 days) exerts CDH6-dependent cell growth-inhibitory activity, potently inhibiting growth of CDH6-positive NIH:OVCAR-3 and PA-1 ovarian cancer cells, while having no effect on CDH6-negative ES-2 ovarian cancer cells[1].
Raludotatug deruxtecan (R-DXd) (0.001-1000 ng/mL; 6 days) exerts CDH6-dependent cell growth-inhibitory activity, as its cytotoxic effect is abrogated in CDH6-knockout NIH:OVCAR-3 cells despite preserved sensitivity to free DXd[1].
Raludotatug deruxtecan (R-DXd) (10 ng/mL; 6, 8, or 10 days) exhibits a bystander antitumor effect, where payload released from CDH6-positive cells diffuses to kill adjacent CDH6-negative cells[1].
Raludotatug deruxtecan (R-DXd) (3 μg/mL; 3 days) induces DNA damage and apoptosis in CDH6-positive PA-1 ovarian cancer cells[1].
Raludotatug deruxtecan (R-DXd) (10 nmol/L; 0, 0.5, 1, 3, 6, 12, 24, or 48 hours at 37°C) exhibits high internalization efficiency in CDH6-positive NIH:OVCAR-3 ovarian cancer cells, with nearly complete internalization within 24 hours[1].
Raludotatug deruxtecan (R-DXd) (10 nmol/L; 0, 0.5, 1, 3, 6, 12, 24, or 48 hours at 37°C) reduces cell-surface CDH6 expression in CDH6-positive NIH:OVCAR-3 ovarian cancer cells, but CDH6 expression recovers rapidly if unbound R-DXd is removed from the medium[1].
Raludotatug deruxtecan (R-DXd) (10 μg/mL; up to 24 hours at 37°C) binds to CDH6 at cell-cell boundaries, is internalized, and traffics to lysosomes in CDH6-expressing CHO-K1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CDH6-positive human ovarian cancer cell lines (NIH:OVCAR-3, PA-1) and CDH6-negative human ovarian cancer cell line (ES-2)
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Concentration:0.001-1000 ng/mL
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Incubation Time:6 days
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Result:Potently inhibited growth of CDH6-positive NIH:OVCAR-3 and PA-1 cells. Showed no growth-inhibitory activity against CDH6-negative ES-2 cells.
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Cell Line:Parental CDH6-positive NIH:OVCAR-3 cells and CDH6-knockout NIH:OVCAR-3 (KO-OVCAR-3) cells
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Concentration:0.001-1000 ng/mL
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Incubation Time:6 days
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Result:Potently inhibited growth of parental NIH:OVCAR-3 cells. Showed severely weakened growth-inhibitory activity against KO-OVCAR-3 cells (which retain sensitivity to free DXd).
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Cell Line:CDH6-positive PA-1 human ovarian cancer cells
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Concentration:3 μg/mL
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Incubation Time:3 days
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Result:Induced phosphorylation of Chk1 (a DNA damage marker). Induced cleavage of caspase-3 (an apoptosis marker).
Raludotatug Deruxtecan (10 mg/kg; i.v.; days 0 and 21) induces significant tumor regression in CDH6-positive ovarian and renal cell carcinoma patient-derived xenograft models, but not in CDH6-negative models[1].
Raludotatug Deruxtecan (3 mg/kg; i.v.; single dose on day 0 for PA-1 models; 10 mg/kg; i.v.; single dose on day 0 for JHOC-5 models) exhibits equivalent antitumor efficacy in parental and sCDH6-overexpressing ovarian cancer xenografts, indicating sCDH6 does not inhibit its activity[1].
Raludotatug Deruxtecan (10-80 mg/kg; i.v.; once every 3 weeks for 6 weeks for 10, 30 mg/kg; single dose for 80 mg/kg) has a highest non-severely toxic dose of 30 mg/kg in cynomolgus monkeys, with mild-to-moderate, mostly reversible toxicity observed at this dose[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CAnN.Cg-Foxn1^nu/CrlCrlj (female, 4 to 5 weeks old)[1]
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Dosage:0.25-10 mg/kg (single dose)
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Administration:i.v.; single dose on day 0
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Result:Induced tumor regression in NIH:OVCAR-3 xenografts with final tumor volumes near 0 mm3 at 3 mg/kg. Induced tumor regression in 786-O xenografts, but showed no significant effect on CDH6-negative ES-2 xenografts at 10 mg/kg.
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Animal Model:CAnN.Cg-Foxn1^nu/CrlCrlj (female, 4 to 5 weeks old)[1]
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Dosage:10 mg/kg
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Administration:i.v.; single dose
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Result:Induced tumor regression in carboplatin- and paclitaxel-refractory NIH:OVCAR-3 xenografts with final tumor volumes near 0 mm3. Caused no serious body weight loss.
Chemical Information
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CAS No. 2610074-57-0
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Appearance Liquid
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Color Colorless to light yellow
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SMILES
[Raludotatug Deruxtecan]
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Synonyms
R-DXd; DS-6000
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Shipping
Shipping with dry ice.
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Storage
-80°C, protect from light
Purity & Documentation
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Data Sheet (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Raludotatug Deruxtecan Related Classifications
HY-164734 Related Classifications
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