Atezolizumab-MMAE

Name: Atezolizumab-MMAE
Brand: MedChemExpress
SKU: HY-171572
Rating: 4.5 (0 reviews)

製品番号: HY-171572 純度: 98.04%: Data Sheet SDS COA 取扱説明書
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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 構造式

容量	価格（税別）	在庫状況	数量
500 μg	$1250	在庫あり	Estimated Time of Arrival: December 31
1 mg	$2000	在庫あり	Estimated Time of Arrival: December 31
5 mg		お問い合わせ
10 mg		お問い合わせ

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製品説明

体外実験

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.

体内実験

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]

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: 98.04%

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データシート (270 KB) SDS (251 KB)

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取扱説明書 (2659 KB)

参考文献

[1]. Xiao D, et al. Development of bifunctional anti-PD-L1 antibody MMAE conjugate with cytotoxicity and immunostimulation. Bioorg Chem. 2021 Nov; 116:105366. [Content Brief]

[2]. Zanello A, et al. Anti-PD-L1 immunoconjugates for cancer therapy: Are available antibodies good carriers for toxic payload delivering? Front Pharmacol. 2022 Aug 16; 13:972046.