Sacituzumab tirumotecan
Based on 1 publication(s) in Google Scholar
Sacituzumab tirumotecan (SKB264) is an antibody-drug conjugate and TROP2-directed, topoisomerase I inhibitor payload-delivering agent, with a TROP2 EC50 of 2.787 ng/mL, TROP2 Kd of 0.3083 nM, and topoisomerase I IC50 of 0.7 μM. Sacituzumab tirumotecan is composed of the humanized anti-TROP2 antibody Sacituzumab (HY-P99045), the drug-linker conjugate for ADC is TL033 TFA (HY-147340A). 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
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Sacituzumab tirumotecan
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Biological Activity
Description
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TROP2 2.787 ng/mL (EC50) |
TROP2 0.3083 nM (Kd) |
In Vitro
Sacituzumab tirumotecan (SKB264) 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. Further protocols information, click here.
Parmacokinetics
In Vivo
Sacituzumab tirumotecan (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 (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 (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 (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
Publications (1)
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Journal Impact Factor
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Most Recent
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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
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Keywords
- 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