[CAS NO. 1616385-51-3] Bezuclastinib

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PRODUCTS SPECIFICATIONS [1616385-51-3]

Catalog

HY-145557

Brand

MCE

CAS

1616385-51-3

DESCRIPTION [1616385-51-3]

Overview

MDL	-
Molecular Weight	331.37
Molecular Formula	C19H17N5O
SMILES	O=C(C1=NNC(C)=C1C)NC2=CN=C3NC(C4=CC=CC=C4)=CC3=C2

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

Summary

Bezuclastinib (CGT9486; PLX 9486) is a potent inhibitor of c-kit and c-kit D816V (0.0001< IC ₅₀ <1 μM; extracted from patent WO2014100620 A2, compound P-2007). Bezuclastinib is a tyrosine kinase inhibitor ^[1] ^[2] .

IC50 & Target

c-Kit

<1 μM (IC ₅₀ )

c-kit D816V

<1 μM (IC ₅₀ )

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02401815	Cogent Biosciences, Inc.\|Plexxikon	Gastrointestinal Stromal Tumors	March 6, 2015	Phase 1\|Phase 2
NCT05208047	Cogent Biosciences, Inc.	Advanced Gastrointestinal Stromal Tumors\|Metastatic Cancer	April 14, 2022	Phase 3
NCT05186753	Cogent Biosciences, Inc.	SSM\|Mastocytosis, Indolent\|Mastocytosis, Systemic\|Mastocytosis	October 26, 2021	Phase 2
NCT04996875	Cogent Biosciences, Inc.	Advanced Systemic Mastocytosis (AdvSM)\|SM With an Associated Hematologic Neoplasm (SM-AHN)\|Mast Cell Leukemia (MCL)\|Aggressive Systemic Mastocytosis (ASM)	November 9, 2021	Phase 2

Appearance

Solid

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)

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
10 mM	0.3018 mL	1.5089 mL	3.0178 mL

* Please refer to the solubility information to select the appropriate solvent.