2. Cell Cycle/DNA Damage
  3. Checkpoint Kinase (Chk)
  4. BEN-28010

BEN-28010 is a selective, orally active, blood-brain barrier permeable CHK1 inhibitor with an IC50 of 4.0 nM. BEN-28010 functions as a radiosensitizer, exhibits antitumor efficacy in GBM models. BEN-28010 can be used for the research of glioblastoma.

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

BEN-28010

BEN-28010 Chemical Structure

CAS No. : 3033961-38-2

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

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

BEN-28010 Related Antibodies

Top Publications Citing Use of Products

View All Checkpoint Kinase (Chk) Isoform Specific Products:

View All Isoforms
Chk1 Chk2 BUBR1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

BEN-28010 is a selective, orally active, blood-brain barrier permeable CHK1 inhibitor with an IC50 of 4.0 nM. BEN-28010 functions as a radiosensitizer, exhibits antitumor efficacy in GBM models. BEN-28010 can be used for the research of glioblastoma[1].

IC50 & Target[1]

Chk1

4.0 nM (IC50)

In Vitro

BEN-28010 potently inhibits recombinant human CHK1 kinase with an IC50 of 4.0 ± 0.9 nM[1].
BEN-28010 inhibits CHK1 activity in SW620 cells with an IC50 of 0.45 ± 0.08 μM[1].
BEN-28010 inhibits p53 mutant LN-18 cell viability, with 24-fold greater potency in p53 mutant LN-18 cells (IC50 0.14 ± 0.01 μM) than p53 wild-type A172 cells (IC50 3.3 ± 0.15 μM); it also shows enhanced activity in p53-deficient GBM cell lines overall, and has an IC50 of 99 ± 4 nM in LN229 cells[1].
BEN-28010 potentiates the cytotoxic effects of ionizing radiation in patient-derived GBM stem cells, with an IC50 of 0.62 μM post-3 Gy IR and a therapeutic interaction (RIR > 1)[1].
BEN-28010 has a favorable in vitro ADME and selectivity profile, including high CHK1 selectivity over the kinome and CHK2, low cardiac arrhythmia risk, minimal CYP interactions, high permeability, and low efflux by MDR1 and BCRP[1].

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

BEN-28010 Related Antibodies
In Vivo

BEN-28010 (50-100 mg/kg; p.o.; every other day for 10 days) as monotherapy and in combination with IR produces statistically significant tumor growth inhibition in subcutaneous LN229 GBM xenografts[1].

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

Animal Model: NOD/SCID (female)[1]
Dosage: 15 mg/kg; 50 mg/kg; 100 mg/kg
Administration: p.o.; every other day for 10 days
Result: Resulted in statistically significant reductions in mean tumor volumes compared to vehicle control on day 18 at 50 mg/kg (p=0.0005) and 100 mg/kg (p<0.0001) as monotherapy.
Resulted in statistically significant reductions in average tumor volumes compared to radiotherapy alone on day 21 at 50 mg/kg (p=0.0006) and 100 mg/kg (p<0.0001) in combination with IR.
Molecular Weight

374.44

Formula

C20H22N8
CAS No.
SMILES

CN(C)[C@H](CC1)CN1C(C=C2)=CC=C2N(C=N3)C=C3NC4=NC=C(C#N)N=C4
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.

BEN-28010 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:

BEN-280103033961-38-2BEN28010BEN 28010Checkpoint Kinase (Chk)γH2AXGBM modelsCHK2SW620 cellsCHK1p53-deficient cellsLN-18 cellsAsp94pCHK1(Ser345)glioblastomaInhibitorinhibitorinhibit

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:
BEN-28010
Cat. No.:
HY-186085
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)

Request for HNMR Report

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