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

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.

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Atezolizumab-MMAE Chemical Structure

Atezolizumab-MMAE Chemical Structure

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Description

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].

In Vitro

Atezolizumab-MMAE (Compound 3) (4 µg/mL, 0.5-24 h) can bind to the PD-L1 antigen on the cells membrane and be internalized and transported to lysosomes within 30 min in MDA-MB-231 cells[1].
Atezolizumab-MMAE (0.725-200000 pmol/L, 3 days) has a potent tumor cell inhibitory activity (EC50 of 10.33, 9.75 and 11.94 nM for PD-L1 + MDA-MB-231, PC 9 and A431 cells, respectively) while a weak effect on PD-L1 - Romas cells (EC50: 129.4 nM)[1].
Atezolizumab-MMAE (0.625-10 μg/mL, 48 h) mediates inhibition of the PD1 and PD-L1 interaction and significantly increases levels of IFN-γ when co-cultures with PBMCs[1].

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

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.
In Vivo

Atezolizumab-MMAE (Compound 3) (3 mg/kg, i.p., 2 times per week for 3  weeks) has a potent anti-tumor effect (68% tumor inhibition and 60% tumor regression) compared to Atezolizumab alone in MC38 xenograft PD-1-humanized immune system mice model [1].

MedChemExpress (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.
Appearance

Liquid

SMILES

[Atezolizumab-MMAE]

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Shipping with dry ice.

Storage

-80°C, protect from light

Purity & Documentation
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Help & FAQs
  • 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.

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Atezolizumab-MMAE
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HY-171572
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