2. Apoptosis Antibody-drug Conjugate/ADC Related
  3. Apoptosis ADC Cytotoxin
  4. Anticancer agent 81

Anticancer agent 81 (Compound 37b3) 是一种抗癌剂，能诱导肿瘤细胞周期阻滞和凋亡 (apoptosis)。Anticancer agent 81 可作为有效载荷与 Trastuzumab (HY-P9907) 结合得到抗体偶联活性分子 (ADC) T-PBA。T-PBA 维持了 Trastuzumab 的靶向模式和内化能力。

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Anticancer agent 81 Chemical Structure

Anticancer agent 81 Chemical Structure

CAS No. : 2820286-56-2

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Anticancer agent 81 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

Anticancer agent 81 (Compound 37b3) is an anticancer agent and can induce tumor cell cycle arrest and apoptosis. Anticancer agent 81 can be used as a payload to conjugate with Trastuzumab (HY-P9907) to obtain the antibody–agent conjugate (ADC) T-PBA. T-PBA maintained its mode of target and internalization ability of Trastuzumab[1].

体外研究
(In Vitro)

Anticancer agent 81 (Compound 37b3) (72 h) shows cytotoxicity against SKOV3, MDA-MB-231 and NCI-N87 cells[1].
Anticancer agent 81 (0-5 μM) induces DNA interstrand cross-linking[1].
Anticancer agent 81 (0-3 nM; 24 h) arrests SKOV3 cell cycle at the S-phase[1].
Anticancer agent 81 (0-3 nM; 48 h) induces SKOV3 cell apoptosis[1].
Anticancer agent 81 (25 nM; 12 h) acts on DNA in the nucleus after entering SKOV3 cells and MDA-MB-231 cells[1].
Anticancer agent 81 induces DDR signaling pathways via cross-linking DNA and then activates the caspase cascade and PARP, finally leading to cell cycle arrest and apoptosis[1].
Anticancer agent 81 covalently binds to the DNA sequences and acts on the major groove of DNA[1].

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

Anticancer agent 81 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: SKOV3, MDA-MB-231 and NCI-N87
Concentration:
Incubation Time: 72 h
Result: Showed cytotoxicity with IC50s of 0.17 ± 0.07, 0.90 ± 0.11 and 0.94 ± 0.14 nM against SKOV3, MDA-MB-231 and NCI-N87 cells, respectively.

Cell Cycle Analysis[1]

Cell Line: SKOV3
Concentration: 0.33, 1 and 3 nM
Incubation Time: 24 h
Result: Inhibited the cell cycle at the S-phase.

Apoptosis Analysis[1]

Cell Line: SKOV3
Concentration: 0.33, 1 and 3 nM
Incubation Time: 48 h
Result: Induced cell apoptosis in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: SKOV3 and NCI-N87
Concentration: 0.02, 0.1, 0.5, 2.5 and 12.5 nM
Incubation Time: 48 h
Result: Induced the phosphorylation of histone 2AX (γ-H2AX) in a dose-dependent manner. Induced the cleavage of PARP (cPARP) and caspase 3 (cCas3) in a concentration-dependent manner.
体内研究
(In Vivo)

T-PBA (1-10 mg/kg; i.v.; every 3 days for 4 times) could significantly delay tumor growth in two Her2-positive xenograft models in mice without obvious toxicity and side effects, and the effect is better than Trastuzumab[1].

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

Animal Model: Female balb/c nude mice, SKOV3 and NCI-N87 tumor model[1]
Dosage: 1, 5 and 10 mg/kg
Administration: Tail vein injection on days 0, 3, 6, and 9
Result: Inhibited tumor growth in a dose-dependent manner (57.5% inhibition at 1 mg/kg, 70.0% inhibition at 5 mg/kg, and 91.5% inhibition at 10 mg/kg in SKOV3 tumor model; the tumor growth inhibitory rate was 50.2% for 1 mg/kg, 88.0% for 5 mg/kg, and 97.1% for 10 mg/kg in NCI-N87 tumor model) without obvious side effects.
分子量

762.89

Formula

C46H46N6O5
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
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

Anticancer agent 81 相关分类

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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.

Keywords:

Anticancer agent 812820286-56-2Anticancer agent81Anticancer agent-81ApoptosisADC CytotoxinADC PayloadanticancerTrastuzumabSKOV3NCI-N87MDA-MB-231Inhibitorinhibitorinhibit

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