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

Bezuclastinib  (Synonyms: CGT9486; PLX 9486)

Cat. No.: HY-145557 Purity: 98.81%
Handling Instructions Technical Support

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).

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Bezuclastinib

Bezuclastinib 화학구조

CAS No. : 1616385-51-3

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
1 mg 해외재고보유
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Bezuclastinib

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

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
분자량

331.37

화학식

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

선적

Room temperature in continental US; may vary elsewhere.

보관

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)

용액&용해도
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.

  • 몰농도 계산기

  • 농도 희석 계산기

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
순도&문서

Purity: 98.81%

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
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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.

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Inquiry Information

상품명:
Bezuclastinib
Cat. No.:
HY-145557
수량:
MCE Japan Authorized Agent: