2. Cell Cycle/DNA Damage Stem Cell/Wnt Protein Tyrosine Kinase/RTK
  3. Casein Kinase FLT3 CDK
  4. SR-2890

SR-2890 is a highly selective, ATP-competitive inhibitor of casein kinase CK1δ and CK1ε, with IC50 values ​​of 4 nM and 44 nM, respectively, and a Ki of 14 nM for CK1δ. SR-2890 exhibits antiproliferative effects. SR-2890 blocks the serine/threonine kinase activity of CK1δ and weakly inhibits a few off-target kinases such as FLT3, CDK4. SR-2890 has an oral bioavailability of 10% and a blood-brain barrier penetration rate of <1%. SR-2890 demonstrates stable in vitro metabolism and favorable in vivo pharmacokinetic properties, effectively inhibiting the growth of human A375 melanoma cells. SR-2890 can be used in melanoma research and is also a useful compound for studying CK1δ/ε-related diseases such as Alzheimer's disease.

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

SR-2890

SR-2890 Chemical Structure

CAS No. : 1454584-91-8

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.

SR-2890 Related Antibodies

Top Publications Citing Use of Products

View All Casein Kinase Isoform Specific Products:

View All Isoforms
CK1 CK2

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SR-2890 is a highly selective, ATP-competitive inhibitor of casein kinase CK1δ and CK1ε, with IC50 values ​​of 4 nM and 44 nM, respectively, and a Ki of 14 nM for CK1δ. SR-2890 exhibits antiproliferative effects. SR-2890 blocks the serine/threonine kinase activity of CK1δ and weakly inhibits a few off-target kinases such as FLT3, CDK4. SR-2890 has an oral bioavailability of 10% and a blood-brain barrier penetration rate of <1%. SR-2890 demonstrates stable in vitro metabolism and favorable in vivo pharmacokinetic properties, effectively inhibiting the growth of human A375 melanoma cells. SR-2890 can be used in melanoma research and is also a useful compound for studying CK1δ/ε-related diseases such as Alzheimer's disease[1].

IC50 & Target

CK1δ

4 nM (IC50)

CK1ε

44 nM (IC50)

Cdk4/cyclin D1

283 nM (IC50)

Cdk4/cyclin D3

368 nM (IC50)

CK1ε

14 nM (Ki)

In Vitro

SR-2890 inhibits proliferation of human A375 melanoma cells (EC50 = 38 nM)[1].
SR-2890 exhibits human liver microsome stability, solubility, without CYP inhibition (T1/2 = 44 min; solubility = 60 μM; CYP inhibition >10 μM)[1].
SR-2890 weakly inhibits off-target kinases FLT3 (IC50=809 nM), CDK4/cyclin D1 (IC50=283 nM) and CDK4/cyclin D3 (IC50=368 nM)[1].

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

SR-2890 Related Antibodies
Parmacokinetics
Species Dose Route Cmax CL AUC T1/2 F
Mice[1] 1 nM i.v. 4.6 μM 8.4 mL/min/kg 4.16 μM·h 1.50 h 10 %
Molecular Weight

477.92

Formula

C23H21ClFN9
CAS No.
SMILES

FC1=CC(N2C=NC3=C(NCC4=NC5=CC(Cl)=CC=C5N4)N=C(N6CCNCC6)N=C23)=CC=C1
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.

SR-2890 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:

SR-28901454584-91-8SR2890SR 2890Casein KinaseFLT3CDKCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Cyclin dependent kinaseCK1εhuman A375 melanoma cellsCYP inhibitionCDK4/cyclin D1solubilitycasein kinase 1εCK1δcasein kinase 1δhuman liver microsome stabilityhuman cancer cell linesATP-competitiveanimal xenograft studiescancer cellsmelanomaInhibitorinhibitorinhibit

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:
SR-2890
Cat. No.:
HY-123859
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.