Referencia número: HY-101561

Avapritinib

(Synonyms: BLU-285)

14 Cited Publications

Revisión del cliente

Based on 14 publication(s) in Google Scholar

Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC₅₀s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2.

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Pureza: 99.75%
No. CAS: 1703793-34-3
Fòrmula: C₂₆H₂₇FN₁₀
Peso molecular:498.56

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Avapritinib Chemical Structure

No. CAS: 1703793-34-3

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Use of MCE Products

Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (14)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

IC50: 0.27 nM (KIT D816V), 0.24 nM (PDGFRA D842V)^[1]

Ver todos los productos específicos de isoformas PDGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	4.075 μM Compound: 5; BLU-285	Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay	[PMID: 30204441]

In Vitro

Avapritinib (BLU-285) has demonstrated biochemical in vitro activity on the KIT exon 17 mutant enzyme, KIT D816V (IC₅₀=0.27 nM). Cellular activity of Avapritinib on KIT D816 mutants is measured by autophosphorylation in the human mast cell leukemia cell line HMC1.2, and the P815 mouse mastocytoma cell line with IC₅₀=4 and 22 nM, respectively. In Kasumi-1 cells, a t(8;21)-positive AML cell line with a KIT exon 17 N822K mutation, Avapritinib potently inhibits KIT N822K mutant autophosphorylation (IC₅₀=40 nM), downstream signaling, as well as cellular proliferation (IC₅₀=75 nM)^[3].

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

In Vivo

In vivo Avapritinib (BLU-285) is well tolerated and has demonstrated dose dependent antitumor efficacy. Complete tumor growth inhibition and ≥75% KIT kinase inhibition is observed with 10 mg/kg once daily, oral dosing of Avapritinib in the aggressive KIT exon 17 mutant driven P815 mastocytoma model grown as a solid tumor allograft as well as in a disseminated model of disease. Disease burden, measured by whole body luciferase imaging (photons/second/mm²), increases 86-fold in the vehicle control animals over the 24 day dosing period with widespread disease detectable in both femurs, the pelvis and circulating in peripheral blood. Avapritinib at both doses (10 or 30 mg/kg orally, once daily) results in a marked reduction of disease burden throughout the study. Avapritinib at either 10 or 30 mg/kg results in tumor regression in all animals with disease abrogation indistinguishable from background signal measurements in several animals by the end of study. Avapritinib is also well tolerated in this in vivo model and has no adverse effects on body weight at either dose^[3].

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

Ensayo clínico

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

Chemical Information

No. CAS 1703793-34-3
Appearance Solid
Peso molecular 498.56
Fòrmula C₂₆H₂₇FN₁₀
Color White to light yellow
SMILES

CN1N=CC(C2=CN3C(C(N4CCN(C5=NC=C([C@@](C)(N)C6=CC=C(F)C=C6)C=N5)CC4)=NC=N3)=C2)=C1
Synonyms

BLU-285
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (14)

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Journal Impact Factor

Cancer Cell

Effective targeting of PDGFRA-altered high-grade glioma with avapritinib. [Abstract]

2025 Apr 14;43(4):740-756.e8. PMID: 40086436
Neuron

Aberrant coupling of glutamate and tyrosine kinase receptors enables neuronal control of brain-tumor growth. [Abstract]

2025 Aug 27:S0896-6273(25)00591-4. PMID: 40897174

Avapritinib purchased from MedChemExpress. Usage Cited in: Neuron. 2025 Aug 27:S0896-6273(25)00591-4. [Abstract]

Avapritinib treatment (50 mg/kg/day) was administered. Representative immunohistochemistry images of Ki67+ cells were shown.
Acta Pharm Sin B

DeepICER: A deep learning framework for predicting compound-induced gene expression profiles. [Abstract]

2026 May;16(5):2947-2963. PMID: 42180546
Acta Pharm Sin B

2026 Feb.
Biomaterials

Automated discovery of nanomaterials via drug aggregation induced emission. [Abstract]

2022 Oct:289:121800. PMID: 36166893
NPJ Precis Oncol

Clinical and preclinical insights into a novel MDM2::PDGFRA fusion in recurrent glioblastoma. [Abstract]

2025 Aug 16;9(1):289. PMID: 40819143

Avapritinib purchased from MedChemExpress. Usage Cited in: NPJ Precis Oncol. 2025 Aug 16;9(1):289. [Abstract]

PDGFRA D842V phosphorylation and total PDGFRA were assessed following a 2-hour treatment with DMSO (vehicle) or 1, 10, 100 nM concentrations of Avapritinib.

Avapritinib purchased from MedChemExpress. Usage Cited in: NPJ Precis Oncol. 2025 Aug 16;9(1):289. [Abstract]

PDGFRA was treated with Avapritinib, crenolanib, dasatinib, lenvatinib, or ripretinib for 72 h.
Pharmaceuticals (Basel)

Esterase-Responsive Polyglycerol-Based Nanogels for Intracellular Drug Delivery in Rare Gastrointestinal Stromal Tumors. [Abstract]

2023 Nov 16;16(11):1618. PMID: 38004483
Int J Mol Sci

Interaction of Avapritinib with Congo Red in Pancreatic Cancer Cells: Molecular Modeling and Biophysical Studies. [Abstract]

2025 Feb 25;26(5):1980. PMID: 40076604

Avapritinib purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Feb 25;26(5):1980. [Abstract]

The cytotoxicity of BLU-258 alone and in aggregates with Congo red (CR-BLU-258) on pancreatic cell lines was assessed using an LDH assay after 48 h of incubation.

Avapritinib purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Feb 25;26(5):1980. [Abstract]

The morphology of the 3D cell cultures of BxPC3 cells was incubated for 48 h with BLU-258 or CR-BLU-258 and without the tested compounds; scale bar = 200 μm.
Bioengineering (Basel)

Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]

2025 Oct 19;12(10):1121. PMID: 41155119
Mol Pharmacol

Influence of Tyrosine Kinase Inhibition on Organic Anion Transporting Polypeptide 1B3-Mediated Uptake. [Abstract]

2022 Jun;101(6):381-389. PMID: 35383108
Biochem Biophys Res Commun

Avapritinib efficacy in primary hepatic neuroendocrine carcinoma with elevated PDGFRA expression: Insights from a PDX model study. [Abstract]

2024 Aug 6:736:150504. PMID: 39121673
bioRxiv

2026 Jun 17.
SSRN

2023 Aug 14.
Seoul National University

2019 Aug.

Solvente y solubilidad

In Vitro:

DMSO : ≥ 83.33 mg/mL (167.14 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

2.0058 mL

10.0289 mL

20.0578 mL

5 mM

0.4012 mL

2.0058 mL

4.0116 mL

10 mM

0.2006 mL

1.0029 mL

2.0058 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 2.5 mg/mL (5.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Protocolo

Animal Administration^[1]

Mice^[1]
A Kasumi-1 luc⁺ AML NOG SCID mouse femoral injection model is used to assess the efficacy of Avapritinib (BLU-285) in KIT exon 17-mutated CBF-AML. Following a 21 day post injection latency period, mice are dosed with Avapritinib orally, once daily at 10 mg/kg or 30 mg/kg through day 45.

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Wu CP, et al. Avapritinib: A Selective Inhibitor of KIT and PDGFRα that Reverses ABCB1 and ABCG2-MediatedMultidrug Resistance in Cancer Cell Lines. Mol Pharm. 2019 Jul 1;16(7):3040-3052. [Content Brief]

[2]. Evans EK, et al. A precision therapy against cancers driven by KIT/PDGFRA mutations. Sci Transl Med. 2017 Nov 1;9(414). pii: eaao1690. [Content Brief]

[3]. Erica Evans, et al. Blu-285, a Potent and Selective Inhibitor for Hematologic Malignancies with KIT Exon 17 Mutations.Blood 2015 126:568.

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0058 mL	10.0289 mL	20.0578 mL	50.1444 mL
	5 mM	0.4012 mL	2.0058 mL	4.0116 mL	10.0289 mL
	10 mM	0.2006 mL	1.0029 mL	2.0058 mL	5.0144 mL
	15 mM	0.1337 mL	0.6686 mL	1.3372 mL	3.3430 mL
	20 mM	0.1003 mL	0.5014 mL	1.0029 mL	2.5072 mL
	25 mM	0.0802 mL	0.4012 mL	0.8023 mL	2.0058 mL
	30 mM	0.0669 mL	0.3343 mL	0.6686 mL	1.6715 mL
	40 mM	0.0501 mL	0.2507 mL	0.5014 mL	1.2536 mL
	50 mM	0.0401 mL	0.2006 mL	0.4012 mL	1.0029 mL
	60 mM	0.0334 mL	0.1671 mL	0.3343 mL	0.8357 mL
	80 mM	0.0251 mL	0.1254 mL	0.2507 mL	0.6268 mL
	100 mM	0.0201 mL	0.1003 mL	0.2006 mL	0.5014 mL

Keywords

Avapritinib

14 Cited Publications

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Avapritinib

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Publications Citing Use of MedChemExpress (MCE) Avapritinib

Ver todos los productos específicos de isoformas PDGFR

Actividad biológica

Chemical Information

Publications (14)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Avapritinib Related Classifications

HY-101561 Related Classifications