2. Antibody-drug Conjugate/ADC Related Immunology/Inflammation
  3. Antibody-Drug Conjugates (ADCs) TROP2
  4. Sacituzumab tirumotecan

Sacituzumab tirumotecan  (Synonyms: SKB264; MK-2870)

製品番号: HY-164789 純度: 97.82%
COA 取扱説明書 Technical Support

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.

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Sacituzumab tirumotecan

Sacituzumab tirumotecan 構造式

CAS 番号 : 2768350-77-0

容量 価格（税別） 在庫状況 数量
1 mg $450 在庫あり
5 mg $1150 在庫あり
10 mg $1850 在庫あり
25 mg $3650 在庫あり
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Sacituzumab tirumotecan 関連抗体

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製品説明

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[1][2][3].

体外実験

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 関連抗体
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞
Cynomolgus Monkey[2] 1 mg/kg i.v. 23.8 h 0.178 h 25.2 μg/mL 787 μg·h/mL 792 μg·h/mL
Cynomolgus Monkey[2] 3 mg/kg i.v. 24.8 h 0.261 h 77.4 μg/mL 2170 μg·h/mL 2250 μg·h/mL
Cynomolgus Monkey[2] 10 mg/kg i.v. / 0.425 h 25.2 μg/mL 8550 μg·h/mL 8640 μg·h/mL
体内実験

Sacituzumab tirumotecan (SKB264) (1-10 mg/kg; i.v.; twice weekly; 6 times) exhibits dose-dependent antitumor efficacy in the HCC1806 breast cancer CDX model, with TGI ranging from 75.6% to 105.0% at tested doses[2].
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.

Animal Model: BALB/c nude (female)[2]
Dosage: 1, 3, 10 mg/kg
Administration: i.v.; twice weekly; 6 times
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.
Animal Model: BALB/c nude (female)[2]
Dosage: 0.3, 1, 3 mg/kg
Administration: i.v.; twice weekly; 6 times
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.
Animal Model: BALB/c nude[2]
Dosage: 0.5, 1.5, 5 mg/kg
Administration: i.v.; twice weekly; 6 times
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.
Animal Model: NCG[2]
Dosage: 1, 3, 10 mg/kg
Administration: i.v.; twice weekly; 6 times
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.
分子量

157907 (average)

CAS 番号
Appearance

Liquid

Color

Colorless to light yellow

SMILES

[Sacituzumab tirumotecan]
輸送条件

Shipping with dry ice.
保管条件

-80°C, protect from light
純度とドキュメンテーション

純度: 97.82%

COA (231 KB) Others (112 KB) SEC-HPLC (205 KB)

取扱説明書 (2659 KB)
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Sacituzumab tirumotecan Related Classifications

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Keywords:

Sacituzumab tirumotecan2768350-77-0SKB264 MK-2870SKB 264SKB-264MK2870MK 2870MK-2870Antibody-Drug Conjugates (ADCs)TROP2Antibody-Drug ConjugatesEGP-1M1S1GA733-1cynomolgus monkeysDNA damagetopoisomerase Inon-small cell lung cancerTROP2-positive tumor cellsapoptosisG2/S cell cycle arrestHR+/HER2? breast cancermetastatic triple-negative breast cancerInhibitorinhibitorinhibit

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