2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Kinesin Apoptosis
  4. AZD4877

AZD4877 is another isostere to Ispinesib (HY-50759)and also a kinesin spindle protein (Eg5) inhibitor with IC50 of 2 nM.AZD4877 arrests cell mitosis, leads to the formation of the monopolar spindle phenotype and induces apoptosis. AZD4877 inhibits circulating peripheral blood mononuclear cells (PBMCs) and has anti-cancer activity.

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AZD4877 Chemical Structure

AZD4877 Chemical Structure

CAS No. : 758722-49-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of AZD4877:

AZD4877 Related Antibodies

Top Publications Citing Use of Products

View All Kinesin Isoform Specific Products:

View All Isoforms
Kinesin-5/Eg5/KSP Kinesin-6 Kinesin-7/CENP-E Kinesin-12 Kinesin-14

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AZD4877 is another isostere to Ispinesib (HY-50759)and also a kinesin spindle protein (Eg5) inhibitor with IC50 of 2 nM.AZD4877 arrests cell mitosis, leads to the formation of the monopolar spindle phenotype and induces apoptosis. AZD4877 inhibits circulating peripheral blood mononuclear cells (PBMCs) and has anti-cancer activity[1][2][3][4][5].

IC50 & Target

IC50: 2 nM (Eg5)[5]
Cellular Effect
Cell Line Type Value Description References
COLO 205 IC50
0.002 μM
Compound: 65
Anticancer activity against human COLO205 cells after 72 hrs by MTS/PMS assay
Anticancer activity against human COLO205 cells after 72 hrs by MTS/PMS assay
[PMID: 21899292]
COLO 205 IC50
0.003 μM
Compound: 1, AZD-4877
Anticancer activity against human COLO205 cells after 72 hrs by MTS/PMS assay
Anticancer activity against human COLO205 cells after 72 hrs by MTS/PMS assay
[PMID: 21899292]
In Vitro

AZD4877 (10 nM, 24 or 48 hours) induces apoptosis in human bladder cancer cells and AZD4877-sensitive cells generally expressed high levels of p63[2].

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

AZD4877 Related Antibodies

Apoptosis Analysis[2]

Cell Line: UC1, UC3, UC6, UC12, UC15, RT4,JB,BV, T24 cell line
Concentration: 10 nM
Incubation Time: 24 or 48 hours
Result: Induced apoptosis in human bladder cancer cells
In Vivo

AZD4877 (i.v., 6 mg/kg, 12 mg/kg; single dose) has a significant reduction in cell viability and increase in cleaved caspase 3 levels by 48 h post dose in a rat hollow fiber model[1].
AZD4877 (i.v., 6 mg/kg; single dose) shows a T1/2 of 3.5 h, and CL of 36 mL/min/kg in Hans Wistar rats[1].

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

503.66

Formula

C28H33N5O2S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(N(C(C(C)C)C1=NC2=C(C(N1CC3=CC=CC=C3)=O)C(C)=NS2)CCCN)C4=CC=C(C)C=C4
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 : 50 mg/mL (99.27 mM; ultrasonic and warming and heat to 60°C; 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 1.9855 mL 9.9273 mL 19.8547 mL
5 mM 0.3971 mL 1.9855 mL 3.9709 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
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Concentration
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Volume
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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (9.93 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 5 mg/mL (9.93 mM); Clear solution

    This protocol yields a clear solution of ≥ 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 (50.0 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 1.9855 mL 9.9273 mL 19.8547 mL 49.6367 mL
5 mM 0.3971 mL 1.9855 mL 3.9709 mL 9.9273 mL
10 mM 0.1985 mL 0.9927 mL 1.9855 mL 4.9637 mL
15 mM 0.1324 mL 0.6618 mL 1.3236 mL 3.3091 mL
20 mM 0.0993 mL 0.4964 mL 0.9927 mL 2.4818 mL
25 mM 0.0794 mL 0.3971 mL 0.7942 mL 1.9855 mL
30 mM 0.0662 mL 0.3309 mL 0.6618 mL 1.6546 mL
40 mM 0.0496 mL 0.2482 mL 0.4964 mL 1.2409 mL
50 mM 0.0397 mL 0.1985 mL 0.3971 mL 0.9927 mL
60 mM 0.0331 mL 0.1655 mL 0.3309 mL 0.8273 mL
80 mM 0.0248 mL 0.1241 mL 0.2482 mL 0.6205 mL
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AZD4877 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:

AZD4877758722-49-5AZD 4877AZD-4877KinesinApoptosisColo205KSP inhibitorEg5rat hollow fiber modelUC3Inhibitorinhibitorinhibit

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