2. Protein Tyrosine Kinase/RTK
  3. c-Kit
  4. Bezuclastinib

Bezuclastinib  (Synonyms: CGT9486; PLX 9486)

Cat. No.: HY-145557 Purity: 98.59%
COA Handling Instructions

Molarity Calculator

Bezuclastinib (CGT9486) is an orally active, highly selective tyrosine kinase inhibitor with potent activity against KIT D816V. Bezuclastinib can be used for the research of nonadvanced systemic mastocytosis (NonAdvSM).

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

Bezuclastinib Chemical Structure

Bezuclastinib Chemical Structure

CAS No. : 1616385-51-3

Size Price Stock Quantity
5 mg USD 550 In-stock
10 mg USD 880 In-stock
25 mg USD 1750 In-stock
50 mg USD 2800 In-stock
100 mg USD 4480 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 1 publication(s) in Google Scholar

Bezuclastinib Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Bezuclastinib (CGT9486) is an orally active, highly selective tyrosine kinase inhibitor with potent activity against KIT D816V. Bezuclastinib can be used for the research of nonadvanced systemic mastocytosis (NonAdvSM)[1].

IC50 & Target[1]

c-Kit

<1 μM (IC50)

c-kit D816V

<1 μM (IC50)

In Vivo

Bezuclastinib (25 mg/kg, p.o., 3 days) shows a brain:plasma ratio of 0.07 in rats[2].

Pharmacokinetic Analysis in Rats[2]

Route Dose (mg/kg) t1/2 (h) Cmax (ng/mL) AUClast (h*ng/mL)
p.o. 25 2.8 2592±364 21509±2558

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

331.37

Formula

C19H17N5O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=NNC(C)=C1C)NC2=CN=C3NC(C4=CC=CC=C4)=CC3=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 80 mg/mL (241.42 mM; Need ultrasonic; 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 3.0178 mL 15.0889 mL 30.1777 mL
5 mM 0.6036 mL 3.0178 mL 6.0355 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 (sealed storage, away from moisture and light). 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 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 (sealed storage, away from moisture and light). 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 3.0178 mL 15.0889 mL 30.1777 mL 75.4444 mL
5 mM 0.6036 mL 3.0178 mL 6.0355 mL 15.0889 mL
10 mM 0.3018 mL 1.5089 mL 3.0178 mL 7.5444 mL
15 mM 0.2012 mL 1.0059 mL 2.0118 mL 5.0296 mL
20 mM 0.1509 mL 0.7544 mL 1.5089 mL 3.7722 mL
25 mM 0.1207 mL 0.6036 mL 1.2071 mL 3.0178 mL
30 mM 0.1006 mL 0.5030 mL 1.0059 mL 2.5148 mL
40 mM 0.0754 mL 0.3772 mL 0.7544 mL 1.8861 mL
50 mM 0.0604 mL 0.3018 mL 0.6036 mL 1.5089 mL
60 mM 0.0503 mL 0.2515 mL 0.5030 mL 1.2574 mL
80 mM 0.0377 mL 0.1886 mL 0.3772 mL 0.9431 mL
100 mM 0.0302 mL 0.1509 mL 0.3018 mL 0.7544 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.

Bezuclastinib 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:

Bezuclastinib1616385-51-3CGT9486 PLX 9486CGT 9486CGT-9486PLX9486PLX 9486PLX-9486c-KitSCFRCD117D816Vtyrosine kinaseNonAdvSMKITInhibitorinhibitorinhibit

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:
Bezuclastinib
Cat. No.:
HY-145557
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.