Sacituzumab tirumotecan
Based on 1 Customer Validation
Sacituzumab tirumotecan is an antibody-drug conjugate and TROP2-directed, topoisomerase I inhibitor payload-delivering agent, with a TROP2 EC50 of 2.787 ng/ml, TROP2 Ka of 0.3083 nM, and topoisomerase I IC50 of 0.7 μmol/L. Sacituzumab tirumotecan can be used for the research of metastatic triple-negative breast cancer, and metastatic non-small cell lung cancer.
For research use only. We do not sell to patients.
- Purity: 97.82%
- CAS No.: 2768350-77-0
- Molecular Weight:157907 (average)
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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
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Biological Activity
Sacituzumab tirumotecan binds to human TROP2 protein with an EC50 of 2.787 ng/ml, similar to its monoclonal antibody[2].
Sacituzumab tirumotecan binds to TROP2-positive HCC1806 and NCI-N87 cells with EC50 values of 11.21 nM and 6.213 nM, respectively[2].
Sacituzumab tirumotecan (72 h) inhibits the growth of TROP2-positive HCC1806, NCI-N87, BxPC-3, Calu-3, and NCI-H23 (TROP2+) cells with IC50 values of 1.281-18.83 nM[2].
Sacituzumab tirumotecan (50 μg/ml; 144 h) is stable in human and cynomolgus monkey plasma, with 70% payload release after 144 h of incubation at 50 μg/ml[2].
Sacituzumab tirumotecan (0.0823-2.22 nM; 120 s association, 600 s dissociation) binds to human TROP2 protein with a Kd value of 0.3083 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Sacituzumab tirumotecan (SKB264) (1-10 mg/kg; i.v.; twice weekly; 6 times) exhibits stronger antitumor efficacy than IMMU-132 at the same doses in the HCC1806 breast cancer CDX model[2].
Sacituzumab tirumotecan (SKB264) (0.3-3 mg/kg; i.v.; twice weekly; 6 times) exhibits dose-dependent antitumor efficacy in the NCI-N87 gastric carcinoma CDX model, with TGI ranging from 78.4% to 151.2% at tested doses[2].
Sacituzumab tirumotecan (SKB264) (0.5-5 mg/kg; i.v.; twice weekly; 6 times) exhibits dose-dependent antitumor efficacy in the BR1282 breast cancer PDX model, with TGI ranging from 44.0% to 104.8% at tested doses[2].
Sacituzumab tirumotecan (SKB264) (1-10 mg/kg; i.v.; twice weekly; 6 times) is effective in TROP2-positive gastric carcinoma PDX models (IHC ≥1+), with TGI >100% at 3 mg/kg in tested positive models[2].
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)[2]
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Dosage:1, 3, 10 mg/kg
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Administration:i.v.; twice weekly; 6 times
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Result:Reported tumor growth inhibition (TGI) of 75.6% (1 mg/kg), 98.5% (3 mg/kg), and 105.0% (10 mg/kg) on day 24 after first dose.\nReported tumor growth inhibition (TGI) of 81.06% (1 mg/kg), 189.46% (3 mg/kg), and 188.86% (10 mg/kg) on day 21 after treatment initiation; these values were higher than corresponding doses of IMMU-132.
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Animal Model:BALB/c nude (female)[2]
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Dosage:0.3, 1, 3 mg/kg
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Administration:i.v.; twice weekly; 6 times
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Result:Reported tumor growth inhibition (TGI) of 78.4% (0.3 mg/kg), 139.2% (1 mg/kg), and 151.2% (3 mg/kg) on day 24 after first dose.
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Animal Model:BALB/c nude[2]
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Dosage:0.5, 1.5, 5 mg/kg
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Administration:i.v.; twice weekly; 6 times
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Result:Reported tumor growth inhibition (TGI) of 44.0% (0.5 mg/kg), 92.6% (1.5 mg/kg), and 104.8% (5 mg/kg) on day 24 after first dose.
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Animal Model:NCG[2]
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Dosage:1, 3, 10 mg/kg
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Administration:i.v.; twice weekly; 6 times
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Result:Achieved tumor growth inhibition (TGI) exceeding 100% at 3 mg/kg in all three TROP2-positive models (0406022, A11068, 0501116); observed no antitumor effect in the TROP2-negative model (A19058) at 3 mg/kg.
Chemical Information
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CAS No. 2768350-77-0
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Appearance Liquid
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Molecular Weight 157907 (average)
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Color Colorless to light yellow
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SMILES
[Sacituzumab tirumotecan]
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Synonyms
SKB264; MK-2870
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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 (270 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
[1]. Ouyang Q, et al. Results of a phase 1/2 study of sacituzumab tirumotecan in patients with unresectable locally advanced or metastatic solid tumors refractory to standard therapies. J Hematol Oncol. 2025;18(1):61. Published 2025 Jun 6. [Content Brief]
[2]. Cheng Y, et al. Preclinical profiles of SKB264, a novel anti-TROP2 antibody conjugated to topoisomerase inhibitor, demonstrated promising antitumor efficacy compared to IMMU-132. Front Oncol. 2022;12:951589. Published 2022 Dec 23. [Content Brief]
[3]. Fang W, et al. Sacituzumab tirumotecan versus docetaxel for previously treated EGFR-mutated advanced non-small cell lung cancer: multicentre, open label, randomised controlled trial. BMJ. 2025;389:e085680. Published 2025 Jun 5. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Sacituzumab tirumotecan Related Classifications
HY-164789 Related Classifications
Powered by Bioz
- Sacituzumab tirumotecan
- 2768350-77-0
- SKB264
- MK-2870
- SKB 264
- SKB-264
- MK2870
- MK 2870
- MK-2870
- Antibody-Drug Conjugates (ADCs)
- TROP2
- cynomolgus monkeys
- DNA damage
- topoisomerase I
- non-small cell lung cancer
- TROP2-positive tumor cells
- apoptosis
- G2/S cell cycle arrest
- HR+/HER2? breast cancer
- metastatic triple-negative breast cancer
- Inhibitor
- inhibitor
- inhibit