Art. -Nr.: HY-152839

Elenestinib

(Synonyms: BLU-263)

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Elenestinib (BLU-263) is an orally active inhibitor of Tyrosine kinase with an IC₅₀ value of 6 nM for KIT D816V. Elenestinib minimally penetrates the blood-brain barrier. Elenestinib can be used in the study of systemic mastocytosis.

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Reinheit: 98.68%
CAS. Nr.: 2505078-08-8
Formel: C₂₇H₂₉FN₁₀O
Molecular Weight:528.58

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Elenestinib Chemical Structure

CAS. Nr.: 2505078-08-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC₅₀: 0.2 nM (KIT D816V)^[1]

In Vitro

Activity of Elenestinib against closely related kinases relative to KIT activity in cells (IC₅₀ (nM))^[3]

PDGFRα	PDGFRß	CSF1R	FLT3	KDR
21	6	161	345	>1000

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

In Vivo

Elenestinib (30 mg/kg, oral gavage, a single dose for 30 h) demonstrates brain penetration with brain to plasma ratio of 0.18 in rats^[3].

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

Animal Model:

Male Sprague Dawley rats^[3]
Dosage:

30 mg/kg
Administration:

oral gavage, a single dose for 30 h
Result:

Showed moderate brain penetration with brain to plasma ratio of 0.18.

Clinical Trial

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

Chemical Information

CAS. Nr. 2505078-08-8
Appearance Solid
Molecular Weight 528.58
Formel C₂₇H₂₉FN₁₀O
Color White to off-white
SMILES

OCCN1C=C(C=N1)C2=CN3N=CN=C(N4CCN(C5=NC=C([C@@](N)(C6=CC=C(C=C6)F)C)C=N5)CC4)C3=C2
Synonyms

BLU-263
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (236.48 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

1.8919 mL

9.4593 mL

18.9186 mL

5 mM

0.3784 mL

1.8919 mL

3.7837 mL

10 mM

0.1892 mL

0.9459 mL

1.8919 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 6.25 mg/mL (11.82 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)
Handling Instructions (2659 KB)

Verweise

[1]. Dave N, et al. Safety and pharmacokinetics of BLU-263, a next-generation KIT inhibitor, in healthy volunteers[C]//Cancer Res (AACR Annual Meeting Abstracts). 2021, 122.

[2]. Chifotides HT, et al. SOHO State of the Art Update and Next Questions: Current and Emerging Therapies for Systemic Mastocytosis. Clin Lymphoma Myeloma Leuk. 2024 Jun 25:S2152-2650(24)00239-8. [Content Brief]

[3]. Guarnieri A, et al. Bezuclastinib is a differentiated KIT inhibitor that exhibits unique selectivity to KIT A-loop mutations, minimal brain penetration, and favorable pharmacokinetic properties in preclinical models[C]//Cancer Research. 615 CHESTNUT ST, 17TH FLOOR, PHILADELPHIA, PA 19106-4404 USA: AMER ASSOC CANCER RESEARCH, 2022, 82(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

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	1.8919 mL	9.4593 mL	18.9186 mL	47.2965 mL
	5 mM	0.3784 mL	1.8919 mL	3.7837 mL	9.4593 mL
	10 mM	0.1892 mL	0.9459 mL	1.8919 mL	4.7297 mL
	15 mM	0.1261 mL	0.6306 mL	1.2612 mL	3.1531 mL
	20 mM	0.0946 mL	0.4730 mL	0.9459 mL	2.3648 mL
	25 mM	0.0757 mL	0.3784 mL	0.7567 mL	1.8919 mL
	30 mM	0.0631 mL	0.3153 mL	0.6306 mL	1.5766 mL
	40 mM	0.0473 mL	0.2365 mL	0.4730 mL	1.1824 mL
	50 mM	0.0378 mL	0.1892 mL	0.3784 mL	0.9459 mL
	60 mM	0.0315 mL	0.1577 mL	0.3153 mL	0.7883 mL
	80 mM	0.0236 mL	0.1182 mL	0.2365 mL	0.5912 mL
	100 mM	0.0189 mL	0.0946 mL	0.1892 mL	0.4730 mL

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Elenestinib

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Membrane Protein-targeted Compound Library

Cytokine Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Elenestinib

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Membrane Protein-targeted Compound Library

Cytokine Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Elenestinib Related Classifications

HY-152839 Related Classifications