2. Cell Cycle/DNA Damage PI3K/Akt/mTOR Epigenetics Protein Tyrosine Kinase/RTK
  3. CDK AMPK PDGFR
  4. Narazaciclib

Narazaciclib  (Synonyms: ON123300)

Cat. No.: HY-12624 Purity: 99.34%
COA Handling Instructions

Narazaciclib (ON123300), a strong and brain-penetrant multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent Narazaciclib causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors. Narazaciclib inhibits CDK6 with an IC50 of 9.82 nM.

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

Narazaciclib Chemical Structure

Narazaciclib Chemical Structure

CAS No. : 1357470-29-1

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 158 In-stock
Solution
10 mM * 1 mL in DMSO USD 158 In-stock
Solid
5 mg USD 144 In-stock
10 mg USD 216 In-stock
50 mg USD 792 In-stock
100 mg USD 1140 In-stock
200 mg   Get quote  
500 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 2 publication(s) in Google Scholar

Narazaciclib Related Antibodies

Top Publications Citing Use of Products

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

View All AMPK Isoform Specific Products:

View All Isoforms
NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1

View All PDGFR Isoform Specific Products:

View All Isoforms
PDGFR PDGFRβ PDGFRα

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Narazaciclib (ON123300), a strong and brain-penetrant[1] multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent Narazaciclib causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors[2]. Narazaciclib inhibits CDK6 with an IC50 of 9.82 nM[3].

IC50 & Target[2][3]

Cdk4/cyclin D1

3.9 nM (IC50)

ARK5

5 nM (IC50)

CDK6/cyclinD1

9.82 nM (IC50)

RET

9.2 nM (IC50)

FYN

11 nM (IC50)

FGFR1

26 nM (IC50)

PDGFRβ

26 nM (IC50)

PI3K-δ

144 nM (IC50)

In Vitro

Narazaciclib (ON123300) inhibits U87 glioma cell proliferation with an IC50 of 3.4±0.1 μM[2]. Narazaciclib (1 and 10 μM) inhibits cell proliferation in a panel of 11 glioma models including a patient-derived model (GBM10)[2].
Narazaciclib (6.3 μM; 1 h) reduces phosphorylation of Akt and its downstream signaling components, P70S6K, 40S rpS6 and Rb S780, yet ON123300 induces Erk activation in U87 cells; both in a dose- and time-dependent manner[2]. ON123300 inhibits PI3Kδ with the IC50 of 144nM[3].

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

Narazaciclib Related Antibodies

Cell Cytotoxicity Assay[2]

Cell Line: U87 glioma cells
Concentration: 0, 4, 8, 12, 16 μM
Incubation Time: 72 hour
Result: Had an IC50 equal to 3.4±0.1 μM.

Western Blot Analysis[2]

Cell Line: U87 cells
Concentration: 6.3 μM
Incubation Time: 1 h
Result: Inhibited phosphorylation of Akt (at S473 site) and its downstream signaling components, P70S6K, 40S ribosomal protein S6 (rpS6) and Rb S780 (decreased to 40.1%; 31.8 %; 60.5%; 54.5% relatively to control), yet increased p-Erk (increased to 120% relative to control).
In Vivo

Narazaciclib (ON123300) decreases p-Akt expression and increases p-Erk activity in brain tumors upon administration at both IV doses of 5 mg/kg and 25 mg/kg in U87 brain tumor-bearing mouse. The half-life (T1/2) is 1.5 h for 5 mg/kg and 25 mg/kg in plasma[2].

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

Animal Model: NIH Swiss nude mice bearing U87 glioma model[2].
Dosage: 5 mg/kg or 25 mg/kg
Administration: IV bolus at a dose of either 5 mg/kg or 25 mg/kg via a tail vein.
Result: The p-Akt rapidly declined and reached nadir values of 73% and 60% of control within 30 min after 5 mg/kg and 25 mg/kg dose levels, respectively.
Clinical Trial
Molecular Weight

429.52

Appearance

Solid

Formula

C24H27N7O
CAS No.
SMILES

N#CC1=CC2=CN=C(NC3=CC=C(N4CCN(C)CC4)C=C3)N=C2N(C5CCCC5)C1=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 : 16.67 mg/mL (38.81 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3282 mL 11.6409 mL 23.2818 mL
5 mM 0.4656 mL 2.3282 mL 4.6564 mL
10 mM 0.2328 mL 1.1641 mL 2.3282 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  0.5% CMC-Na/saline water

    Solubility: 5 mg/mL (11.64 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are available by MedChemExpress (MCE).
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.

Narazaciclib 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.

  • 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

Keywords:

Narazaciclib1357470-29-1ON123300ON 123300ON-123300CDKAMPKPDGFRCyclin dependent kinaseAMP-activated protein kinasePlatelet-derived growth factor receptorRTKkinasebrainpenetrationmultiCDK4CDK6Ark5PDGFRβFGFR1RETFYNtumorU87gliomaInhibitorinhibitorinhibit

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:
Narazaciclib
Cat. No.:
HY-12624
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.