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

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.

For research use only. We do not sell to patients.

Anticancer agent 81 Chemical Structure

Anticancer agent 81 Chemical Structure

CAS No. : 2820286-56-2

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Anticancer agent 81 Related Antibodies

Top Publications Citing Use of Products

View All ADC Cytotoxin Isoform Specific Products:

View All Isoforms
Auristatin Calicheamicins Camptothecins Daunorubicins/Doxorubicins Duocarmycins Maytansinoids Pyrrolobenzodiazepines Traditional Cytotoxic Agents

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

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].

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

Anticancer agent 81 Related Antibodies

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.
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].

MedChemExpress (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.
Molecular Weight

762.89

Formula

C46H46N6O5
CAS No.
SMILES

O=C1N(CCN2CCN(CCCCCOC3=C(OC)C=C4C(N=C[C@@](CC(C5=CC=C(N)C=C5)=C6)([H])N6C4=O)=C3)CC2)C(C7=CC=CC8=CC9=CC=CC=C9C1=C78)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Anticancer agent 81 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Anticancer agent 81
Cat. No.:
HY-151207
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.