2. Antibody-drug Conjugate/ADC Related Cell Cycle/DNA Damage
  3. ADC Payload Topoisomerase
  4. (αR)-Cyclopropaneacetamide-Exatecan

(αR)-Cyclopropaneacetamide-Exatecan  (Synonyms: SHR169265)

Cat. No.: HY-156617A Purity: 99.93%
COA
SDS
Handling Instructions Technical Support

(αR)-Cyclopropaneacetamide-Exatecan (SHR169265) is a DNA Topoisomerase I inhibitor with enhanced membrane permeability (with an IC50 of 1.34 μM against the human DNA Topoisomerase I). (αR)-Cyclopropaneacetamide-Exatecan exerts cytotoxic effects by inhibiting the enzymatic activity of Topoisomerase I, and this anticancer effect is independent of the expression level of HER2. (αR)-Cyclopropaneacetamide-Exatecan is an ADC Cytotoxin derived from Exatecan (HY-13631), which can be used in research related to advanced cancers such as breast cancer, gastric cancer, colorectal cancer and non-small cell lung cancer.

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

(αR)-Cyclopropaneacetamide-Exatecan

(αR)-Cyclopropaneacetamide-Exatecan Chemical Structure

CAS No. : 2414254-37-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

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

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of (αR)-Cyclopropaneacetamide-Exatecan:

(αR)-Cyclopropaneacetamide-Exatecan Related Antibodies

Top Publications Citing Use of Products

View All ADC Payload Isoform Specific Products:

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

View All Topoisomerase Isoform Specific Products:

View All Isoforms
Topoisomerase Topo I Topo II DNA gyrase

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

(αR)-Cyclopropaneacetamide-Exatecan (SHR169265) is a DNA Topoisomerase I inhibitor with enhanced membrane permeability (with an IC50 of 1.34 μM against the human DNA Topoisomerase I). (αR)-Cyclopropaneacetamide-Exatecan exerts cytotoxic effects by inhibiting the enzymatic activity of Topoisomerase I, and this anticancer effect is independent of the expression level of HER2. (αR)-Cyclopropaneacetamide-Exatecan is an ADC Cytotoxin derived from Exatecan (HY-13631), which can be used in research related to advanced cancers such as breast cancer, gastric cancer, colorectal cancer and non-small cell lung cancer[1].
IC50 & Target

Camptothecins

 

In Vitro

SHR169265 exhibits potent, HER2 expression-independent cytotoxicity against 9 human cancer cell lines, with IC50 values ranging from 0.30 nM to 2.32 nM after 6 days of incubation[1].

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

(αR)-Cyclopropaneacetamide-Exatecan Related Antibodies

Cell Viability Assay[1]

Cell Line: NCI-N87, SK-BR-3, HCC1954, JIMT-1, Capan-1, AGS, MKN45, SNU-16, MDA-MB-468
Concentration: Serially diluted concentrations
Incubation Time: 6 days
Result: Induced strong cytotoxicity across all tested cell lines, with IC50 values of 1.00±0.07 nM (NCI-N87), 0.58±0.10 nM (SK-BR-3), 0.55±0.19 nM (HCC1954), 2.32±0.45 nM (JIMT-1), 0.38±0.07 nM (Capan-1), 0.36±0.11 nM (AGS), 0.30±0.07 nM (MKN45), 0.57±0.19 nM (SNU-16), and 0.56±0.09 nM (MDA-MB-468).
Parmacokinetics
Species Dose Route Cmax AUC0-t T1/2 CL Vss
Mice[1] 0.5 mg/kg i.v. 250 ng/mL 113 ng·h/mL 0.37 h 72.6 mL/min/kg 1815 mL/kg
In Vivo

SHR-A1811 (1-6 mg/kg; i.p.; single dose), delivering target reagent SHR169265, induces dose-dependent tumor growth inhibition (85% to 124% TGI) and tumor regression in HER2-high gastric cancer xenografts, with tumoral payload levels correlating with PARP cleavage, a biomarker of apoptosis[1].
SHR-A1811 (1-10 mg/kg; i.p.; single dose; once weekly for 2 doses), delivering target reagent SHR169265, induces dose-dependent tumor growth inhibition (57.9% to 108.8% TGI) in HER2-moderate breast cancer xenografts, with repeated dosing enhancing efficacy[1].
SHR-A1811 (1-6 mg/kg; i.p.; single dose), delivering target reagent SHR169265, induces dose-dependent tumor growth inhibition (91% to 120% TGI) in HER2-low pancreatic cancer xenografts[1].

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

Animal Model: NU/NU nude mice with Gastric cancer (female, 15-18g); Beige SCID mice (female, 15-18g); Balb/c nude mice (female, 15-18g)[1]
Dosage: 1 mg/kg; 3 mg/kg; 6 mg/kg
Administration: i.p.; single dose
Result: Induced 85% TGI at 1 mg/kg.
Induced 124% TGI with sustained tumor regression through day 17 at 3 mg/kg.
Induced 119% TGI with sustained tumor regression through day 17 at 6 mg/kg.
Maintained low and stable tumoral levels at 1 mg/kg.
Reached tumoral Cmax at 24 hours at 3 mg/kg.
Reached tumoral Cmax at 72 hours at 6 mg/kg.
Induced PARP cleavage in tumor cells, with degree correlated with tumoral SHR169265 levels.
Animal Model: NU/NU nude mice with Breast cancer (female, 15-18g); Beige SCID mice (female, 15-18g); Balb/c nude mice (female, 15-18g)[1]
Dosage: 5 mg/kg (single dose); 10 mg/kg (single dose); 1 mg/kg (weekly x2); 3 mg/kg (weekly x2); 6 mg/kg (weekly x2)
Administration: i.p.; single dose; once weekly for 2 doses
Result: Induced 57.9% TGI at 5 mg/kg single dose.
Induced 80.7% TGI at 10 mg/kg single dose.
Induced 91.8% TGI at 1 mg/kg once weekly for 2 doses.
Induced 108.8% TGI at 3 mg/kg once weekly for 2 doses.
Induced 101.4% TGI at 6 mg/kg once weekly for 2 doses.
Molecular Weight

533.55

Formula

C29H28FN3O6
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O[C@H](C1CC1)C(N[C@@H]2C3=C4C(C(N5C4)=CC([C@](O)(C(OC6)=O)CC)=C6C5=O)=NC7=CC(F)=C(C)C(CC2)=C73)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (187.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8742 mL 9.3712 mL 18.7424 mL
5 mM 0.3748 mL 1.8742 mL 3.7485 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8742 mL 9.3712 mL 18.7424 mL 46.8560 mL
5 mM 0.3748 mL 1.8742 mL 3.7485 mL 9.3712 mL
10 mM 0.1874 mL 0.9371 mL 1.8742 mL 4.6856 mL
15 mM 0.1249 mL 0.6247 mL 1.2495 mL 3.1237 mL
20 mM 0.0937 mL 0.4686 mL 0.9371 mL 2.3428 mL
25 mM 0.0750 mL 0.3748 mL 0.7497 mL 1.8742 mL
30 mM 0.0625 mL 0.3124 mL 0.6247 mL 1.5619 mL
40 mM 0.0469 mL 0.2343 mL 0.4686 mL 1.1714 mL
50 mM 0.0375 mL 0.1874 mL 0.3748 mL 0.9371 mL
60 mM 0.0312 mL 0.1562 mL 0.3124 mL 0.7809 mL
80 mM 0.0234 mL 0.1171 mL 0.2343 mL 0.5857 mL
100 mM 0.0187 mL 0.0937 mL 0.1874 mL 0.4686 mL
  • 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.

(αR)-Cyclopropaneacetamide-Exatecan Related Classifications

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:

(αR)-Cyclopropaneacetamide-Exatecan2414254-37-6SHR169265SHR 169265SHR-169265ADC PayloadTopoisomeraseADC Cytotoxinnon-small cell lung cancerDNA topoisomerase Ibreast cancerhuman DNA topoisomerase IHER2C57BL/6 micecolorectal cancercancer cellshuman cancer cell linesgastric cancerInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
(αR)-Cyclopropaneacetamide-Exatecan
Cat. No.:
HY-156617A
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

SAFETY DATA SHEET (SDS)

English - EN (252 KB) Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB) Italian - IT (252 KB) Korean - KR (252 KB) Portuguese - PT (252 KB)

Request for HNMR Report

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