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Cat. No.: HY-145557

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Bezuclastinib

Name: Bezuclastinib
Brand: MedChemExpress
SKU: HY-145557
Price: 220.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: CGT9486; PLX 9486)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

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).

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Pureté: 98.81%
CAS No.: 1616385-51-3
Formule: C₁₉H₁₇N₅O
Masse moléculaire:331.37

Stockage:

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)

Bezuclastinib Chemical Structure

CAS No.: 1616385-51-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vivo
- Essai clinique
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
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Activité biologique

Description

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)	t_1/2 (h)	C_max (ng/mL)	AUC_last (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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1616385-51-3
Appearance Solid
Masse moléculaire 331.37
Formule C₁₉H₁₇N₅O
Color White to off-white
SMILES

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

CGT9486; PLX 9486
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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)

Publications (1)

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Journal Impact Factor

bioRxiv

2026 Mar 25.

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.0178 mL

15.0889 mL

30.1777 mL

5 mM

0.6036 mL

3.0178 mL

6.0355 mL

10 mM

0.3018 mL

1.5089 mL

3.0178 mL

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.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (272 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Guarnieri A, et al. Preclinical Data with KIT D816V Inhibitor Bezuclastinib (CGT9486) Demonstrates High Selectivity and Minimal Brain Penetrance. Blood. 2021, 138: 4595.

[2]. Guarnieri A, et al. Preclinical data identifies bezuclastinib as a differentiated KIT inhibitor with unique selectivity to KIT D816V and minimal evidence of brain penetration. MOLECULAR CANCER THERAPEUTICS. 2021, 20(12).

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Keywords

Bezuclastinib

1 Cited Publications

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Activité biologique
- Description
- IC₅₀ & Target
- In Vivo
- Essai clinique
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
Pureté et documentation
Références

Nom du produit:
Cat. No.:
Quantité:
MCE Japan Authorized Agent:

Nom du produit:
CAS No.:
Species:
Pureté:
Quantité:

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Publications Citing Use of MedChemExpress (MCE) Bezuclastinib

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

Bezuclastinib

Elenestinib

Avapritinib

Imatinib

Velzatinib

c-Kit-IN-1

Ripretinib

Sunitinib

ISCK03

2-Deoxy-D-glucose

Regorafenib

AZD3229

Motesanib

Publications Citing Use of MedChemExpress (MCE) Bezuclastinib

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Bezuclastinib Related Classifications

HY-145557 Related Classifications

Bioz