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

Anetumab ravtansine  (Synonyms: BAY 94-9343)

目录号: HY-141606
技术支持

Anetumab ravtansine (BAY 94-9343) 是一种靶向类玉米蛋白 (maytansinoid) 微管蛋白 (tubulin) 的抗体药物偶联物 (ADC),效力强、具有选择性。Anetumab ravtansine 由 maytansoid 微管蛋白抑制剂 DM4 偶联人抗间皮素抗体组成。Anetumab ravtansine 在患者源性异种移植瘤模型中显示抗肿瘤药效,其效力与在间皮素表达量相关。

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Anetumab ravtansine Chemical Structure

Anetumab ravtansine Chemical Structure

CAS No. : 1375258-01-7

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  • 生物活性

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生物活性

Anetumab ravtansine (BAY 94-9343) is a selective and highly potent antibody-drug conjugate (ADC) to target maytansinoid tubulin. Anetumab ravtansine consists of a human anti-mesothelin antibody conjugated to the maytansinoid tubulin inhibitor DM4. Anetumab ravtansine shows antitumor efficacy correlated with the amount of mesothelin expressed in patient-derived xenograft tumor models[1].

体外研究
(In Vitro)

Anetumab ravtansine (0.01-300 nM; 4 或 24 h) 在间皮素表达细胞中表现出强大的选择性的细胞毒性,IC50 为0.72 nM,但不影响间皮素阴性或非增殖细胞[1]
Anetumab ravtansine 还诱导相邻间皮阴性肿瘤细胞的旁观者效应[1]

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

Cell Viability Assay[1]

Cell Line: MIA PaCa-2 and HT-29; OVCAR-3; and NCI-H226
Concentration: 0.01 nM-300 nM
Incubation Time: 24 hours
Result: Inhibited cell viability with IC50s of 1.59 nM (MIA PaCa-2), 0.715 nM (HT-29), 1.59 nM (OVCAR-3), and 5.72 nM (NCI-H226), respectively.
体内研究
(In Vivo)

Anetumab ravtansine (10 mg/kg; 静脉注射) 特异性定位于间皮阳性肿瘤,显示出抗肿瘤活性;并在皮下和原位异种移植模型中抑制肿瘤生长[1]

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

Animal Model: Subcutaneous and orthotopic xenograft models: MIA PaCa, HT29, OVCAR-3, NCI-H226 and so on (NMRI nu/nu mice: 18-25 g, 7-10 weeks old)[1]
Dosage: 2.7 mg/kg (0.05 mg/kg DM4), 10.6 mg/kg (0.2 mg/kg DM4)
Administration: MF-T, or S-methyl-DM4 on days 5, 8, and 12 (mice implanted with MIA PaCa or HT29 meso cells); on days 33, 36, and 40 (OVCAR-3); on days 78, 81, 84, 127, 130, and 133 (NCI-H226); on days 15, 18, and 22 (OVCAR-3- s-05 orthotopic); on days 7, 10, and 13 (HT29 titration); Q3Dx3 starting on day 0 (PAXF736); Q3Dx3 starting on day 29 (OVCAR6719); or Q4Dx3 starting on day 34 (Meso7212) after tumor cell inoculation.
Result: Resulted in complete tumor eradication at 10.6 mg/kg (0.2 mg/kg DM4), lasting for at least 17 weeks following the final treatment.
Eradicated tumors in 5 out of 6 animals in the MIA PaCa-2/meso model rather than in HT-29/ meso model at 2.7 mg/kg (0.05 mg/kg DM4).
CAS 号
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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Anetumab ravtansine
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HY-141606
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