2. Antibody-drug Conjugate/ADC Related Cytoskeleton Cell Cycle/DNA Damage Apoptosis
  3. Antibody-Drug Conjugates (ADCs) Microtubule/Tubulin Apoptosis
  4. Atezolizumab-MMAE

Atezolizumab-MMAE 是一种抗 PD-L1 抗体-药物偶联物 (ADC)，其 EC50 为 1.1 nM。Atezolizumab-MMAE 由人源化抗 PD-L1 抗体 (Atezolizumab) (HY-P9904)、溶酶体可裂解的二肽连接体 (valine-citrulline)、tubulin 抑制剂 (MMAE) (HY-15162) 组成，且 ADC 的药物-连接体偶联物为 VcMMAE (HY-15575)。Atezolizumab-MMAE 具有强效细胞毒性 (EC50：9.75-11.94 nM) 和免疫激活作用。Atezolizumab-MMAE 在 MC38 异种移植 PD-1 人源化免疫系统小鼠模型中具有显著的抗肿瘤活性。

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Atezolizumab-MMAE

Atezolizumab-MMAE Chemical Structure

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500 μg ￥15120
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Atezolizumab-MMAE 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Atezolizumab-MMAE is an anti-PD-L1 antibody-drug conjugate (ADC) with an EC50 of 1.1 nM. Atezolizumab-MMAE is composed of a humanized anti-PD-L1 antibody (Atezolizumab) (HY-P9904), a lysosomally cleavable dipeptide linker (valine-citrulline), a tubulin inhibitor (MMAE) (HY-15162), and the drug-linker conjugate for ADC is VcMMAE (HY-15575). Atezolizumab-MMAE has a potent cytotoxicity (EC50: 9.75-11.94 nM) and immune activation effect. Atezolizumab-MMAE has a significantly anti-tumor activity in MC38 xenograft PD-1-humanized immune system mice model[1][2].

体外研究
(In Vitro)

Atezolizumab-MMAE (Compound 3) (4 µg/mL, 0.5-24 小时) 可与 MDA-MB-231 细胞中细胞膜上的 PD-L1 抗原结合，并在 30 分钟内被内化并转运至溶酶体[1]。
Atezolizumab-MMAE (0.725-200000 pmol/L，3 天) 具有强效的肿瘤细胞抑制活性 (对 PD-L1 + 的 MDA-MB-231、PC 9 和 A431 细胞的 EC50 分别为 10.33、9.75 和 11.94 nM)，而对 PD-L1 - 的 Romas 细胞的作用较弱 (EC50：129.4 nM)[1]。
Atezolizumab-MMAE (0.625-10 μg/mL，48 小时) 可介导对 PD1 和 PD-L1 相互作用的抑制，并在与 PBMCs 共培养时显著提高 IFN-γ 水平[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Atezolizumab-MMAE 相关抗体:

Cell Viability Assay[1]

Cell Line: MDA-MB-231, PC 9, A431, Romas cells
Concentration: 0.725-200000 pmol/L
Incubation Time: 3 days
Result: Demonstrated a potent inhibitory activity in the MDA-MB-231, PC 9 and A431 PD-L1 + cell lines with EC50 of 10.33 nM, 9.75 nM, and 11.94 nM, respectively.
Exhibited a weak inhibitory activity against the PD-L1 - cell Romas lines with EC50 of 124.9 nM.

Cell Viability Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 4 µg/mL
Incubation Time: 0, 0.5, 1, 4, 18, 24 h
Result: Could bind to the PD-L1 antigen on the membrane of MDA-MB-231 cells at 4 °C.
Be internalized into lysosomes of MDA-MB-231 cells only 30 min.
体内研究
(In Vivo)

Atezolizumab-MMAE (Compound 3) (3 mg/kg，腹腔注射，每周 2 次，持续 3 周) 与单独使用 Atezolizumab 相比，对 MC38 异种移植 PD-1 人源化免疫系统小鼠模型具有更强的抗肿瘤作用 (68% 的肿瘤抑制率和 60% 的肿瘤消退率)[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female C57BL/6J-Pdcd1em1 (hPDCD1)/Smoc mice (6-8 weeks old) were inoculated subcutaneously into the upper groin of the lateral hind limbs with log growth-phase of MC38 cells (1 × 106 cells/mouse)[1].
Dosage: 3 mg/kg
Administration: i.p., 2 times per week for 3  weeks following tumor volume reaching about 50-150 mm3, and then measured tumor volume and body weights twice weekly.
Result: Produced significant and sustained antitumor effects with a 68% tumor inhibition rate.
Significantly disappeared tumor with tumor regression of 60%, which higher than Atezolizumab alone (tumor regression: 40%).
Had a safety profile with no significant body weight changes.
性状

液体

运输条件

Shipping with dry ice.
储存方式

-80°C, protect from light
纯度 & 产品资料
参考文献

Atezolizumab-MMAE 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Atezolizumab-MMAEAntibody-Drug Conjugates (ADCs)Microtubule/TubulinApoptosisAntibody-Drug ConjugatesPD-L1Antibody-drug conjugateADCAntitumorCancer therapyImmunotherapyInhibitorinhibitorinhibit

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