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| ln Vitro |
Sacituzumab tirumotecan binds to human TROP2 protein with an EC50 value 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 hours) 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) was stable in human and cynomolgus monkey plasma, and the effective payload release rate was 70% after incubation at a concentration of 50 μg/ml for 144 hours [2]. Sacituzumab tirumotecan (0.0823–2.22 nM; binding time 120 s, dissociation time 600 s) bound to human TROP2 protein with a Kd value of 0.3083 nM [2].
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| ln Vivo |
Sacituzumab tirumotecan (SKB264) (1-10 mg/kg; intravenous injection; twice a week; for a total of 6 times) showed dose-dependent antitumor efficacy in the HCC1806 breast cancer CDX model, with tumor growth inhibition rate (TGI) ranging from 75.6% to 105.0% at the tested dose [2]. In the HCC1806 breast cancer CDX model, the antitumor efficacy of Sacituzumab tirumotecan (SKB264) (1-10 mg/kg; intravenous injection; twice a week; for a total of 6 times) was stronger than that of IMMU-132 at the same dose [2]. Sacituzumab tirumotecan (SKB264) (0.3-3 mg/kg; intravenous injection; twice a week; for a total of 6 times) showed dose-dependent antitumor efficacy in the NCI-N87 gastric cancer CDX model, with tumor growth inhibition rate (TGI) ranging from 78.4% to 151.2% at the tested dose [2]. Sacituzumab tirumotecan (SKB264) (0.5–5 mg/kg; intravenous injection; twice weekly for a total of 6 times) demonstrated dose-dependent antitumor efficacy in the BR1282 breast cancer PDX model, with tumor growth inhibition rate (TGI) ranging from 44.0% to 104.8% at the tested dose[2]. Sacituzumab tirumotecan (SKB264) (1–10 mg/kg; intravenous injection; twice weekly for a total of 6 times) was effective in the TROP2-positive gastric cancer PDX model (IHC ≥ 1+), with a TGI > 100% at the tested positive model at a dose of 3 mg/kg[2].
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| Animal Protocol |
Animal/Disease Models:BALB/c nude mice (female) [2]
Doses: 1, 3, 10 mg/kg Route of Administration: Intravenous injection; twice a week; 6 times in total Experimental Results: On day 24 after the first administration, the tumor growth inhibition rate (TGI) was 75.6% (1 mg/kg), 98.5% (3 mg/kg), and 105.0% (10 mg/kg), respectively. On day 21 after the start of treatment, the tumor growth inhibition rate (TGI) was 81.06% (1 mg/kg), 189.46% (3 mg/kg), and 188.86% (10 mg/kg), respectively; these values were all higher than the corresponding doses of IMMU-132. Animal/Disease Models:BALB/c nude mice (female) [2] Doses: 0.3, 1, 3 mg/kg Route of Administration: Intravenous injection; twice a week; 6 times in total Experimental Results: On day 24 after the first administration, the tumor growth inhibition rate (TGI) was 78.4% (0.3 mg/kg), 139.2% (1 mg/kg) and 151.2% (3 mg/kg), respectively. Animal/Disease Models:BALB/c nude mice [2] Doses: 0.5, 1.5, 5 mg/kg Route of Administration: Intravenous injection; twice a week; 6 times in total Experimental Results: On day 24 after the first administration, the tumor growth inhibition rate (TGI) was 44.0% (0.5 mg/kg), 92.6% (1.5 mg/kg) and 104.8% (5 mg/kg), respectively. Animal/Disease Models:NCG[2] Doses: 1, 3, 10 mg/kg Route of Administration: Intravenous injection; twice a week; 6 times in total Experimental Results: In all three TROP2 positive models (0406022, A11068, 0501116), the tumor growth inhibition rate (TGI) at a dose of 3 mg/kg exceeded 100%; in the TROP2 negative model (A19058), no antitumor effect was observed at a dose of 3 mg/kg. |
| References |
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| Molecular Weight |
157907 (average)
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| CAS # |
2768350-77-0
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| Appearance |
Colorless to light yellow liquid
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| SMILES |
[Sacituzumab tirumotecan]
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| Synonyms |
SKB264; MK-2870
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: 本产品在运输和储存过程中需避光（避免光照）。 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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