1. Cell Cycle/DNA Damage PI3K/Akt/mTOR Epigenetics Protein Tyrosine Kinase/RTK
  2. CDK AMPK PDGFR
  3. 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 121 In-stock
Solution
10 mM * 1 mL in DMSO USD 121 In-stock
Solid
5 mg USD 110 In-stock
10 mg USD 180 In-stock
50 mg USD 550 In-stock
100 mg USD 800 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

Top Publications Citing Use of Products
  • 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.

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

Formula

C24H27N7O

CAS No.
Appearance

Solid

Color

Yellow to orange

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; 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 2.3282 mL 11.6409 mL 23.2818 mL
5 mM 0.4656 mL 2.3282 mL 4.6564 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:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  0.5% CMC-Na/saline water

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

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.
Calculation results:
Working solution concentration: mg/mL
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 2.3282 mL 11.6409 mL 23.2818 mL 58.2045 mL
5 mM 0.4656 mL 2.3282 mL 4.6564 mL 11.6409 mL
10 mM 0.2328 mL 1.1641 mL 2.3282 mL 5.8205 mL
15 mM 0.1552 mL 0.7761 mL 1.5521 mL 3.8803 mL
20 mM 0.1164 mL 0.5820 mL 1.1641 mL 2.9102 mL
25 mM 0.0931 mL 0.4656 mL 0.9313 mL 2.3282 mL
30 mM 0.0776 mL 0.3880 mL 0.7761 mL 1.9402 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.
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.

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: