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Art. -Nr.: HY-182043

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BLU-654

BLU-654 is an orally active antineoplastic agent and KIT inhibitor. BLU-654 is a highly selective inhibitor targeting wild-type KIT, PDGFRβ, and KIT^V654A over most other kinases in the kinome. BLU-654 exerts sustained antineoplastic activity in KIT^V654A cell-derived xenograft mouse models. BLU-654 can be used in research related to Imatinib (HY-15463)-resistant gastrointestinal stromal tumors.

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CAS. Nr.: 2999638-62-7
Formel: C₂₁H₂₈FN₇O₂
Molecular Weight:429.49

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

BLU-654 Chemical Structure

CAS. Nr.: 2999638-62-7

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle PDGFR Isoform-spezifische Produkte anzeigen :

In Vitro

BLU-654 potently inhibits the autophosphorylation of KIT in HMC1.1 11/13 cells, with an IC₅₀ of 5.7 nM^[1].
BLU-654 inhibits the autophosphorylation of wild-type KIT in M-07e cells with an IC₅₀ of 82.7 nM, and is 15-fold more selective for KIT^V654A than for wild-type KIT^[1].
BLU-654 inhibits the autophosphorylation of PDGFRβ in SW569 cells with an IC₅₀ of 1251.4 nM, and is 219-fold more selective for KIT^V654A than for PDGFRβ^[1].
BLU-654 exhibits species-dependent metabolic stability, with no intrinsic clearance in human and canine liver microsomes, low clearance (2 mL·min^-1·kg^-1) in human hepatocytes, and higher clearance in rat, canine and cynomolgus monkey hepatocytes^[1].

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

Parmacokinetics

Species	Dose	Route	CL_plasma	T_1/2	V_ss	Bioavailability
Rat^[1]	1 mg/kg	i.v.	15.2 mL/min/kg	4.7 h	3.1 L/kg	/
Rat^[1]	5 mg/kg	p.o.	/	/	/	123 %
Cynomolgus Monkey^[1]	0.5 mg/kg	i.v.	4.2 mL/min/kg	2.9 h	1.0 L/kg	/
Dog^[1]	0.5 mg/kg	i.v.	9.0 mL/min/kg	5.3 h	3.7 L/kg	/
Dog^[1]	1.5 mg/kg	p.o.	/	/	/	94.8 %

In Vivo

BLU-654 (1-60 mg/kg; p.o.; once daily; 27 days) demonstrates potent, dose-dependent inhibition of pSTAT5 (a downstream marker of KIT activity) in HMC1.1 11/13 xenografts^[1].

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

Animal Model:

NOD-SCID mice^[1]
Dosage:

1-30 mg/kg (PK/PD); 3-60 mg/kg (Efficacy)
Administration:

p.o.; daily; 27 days (Efficacy); single dose (PK/PD)
Result:

Elicited a dose- and time-dependent reduction in pSTAT5, with a free in vivo IC₅₀ of 4.2 nM at 4 hours.
Reduced pSTAT5 by 95% over 4 hours at 10 mg/kg, with levels returning to 68% of baseline at 24 hours.
Achieved dose-dependent plasma exposures, exceeding the in vitro pKIT IC₅₀ at most doses 10 hours postdosing, and at 30 mg/kg, exposures remained above the in vitro IC₅₀ for up to 24 hours.
Showed slower tumor growth in mice treated with 3 mg/kg compared to controls after 27 days of daily dosing.
Eliminated tumors in mice treated with 10, 30, and 60 mg/kg, with no tumor regrowth observed during the 48-day post-treatment observation period.
Maintained body weight within 10% of baseline across all doses, indicating good tolerability.

Chemical Information

CAS. Nr. 2999638-62-7
Molecular Weight 429.49
Formel C₂₁H₂₈FN₇O₂
SMILES

F[C@@H](C)C1=NC(N)=CC(NC2=NC=C(C3=CN(CC(C)(O)C)N=C3)C(OC(C)C)=C2)=N1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Moine L, et al. Design and Synthesis of BLU-654, a Potent and Selective Mutant KIT V654A Inhibitor for the Treatment of Imatinib-Resistant GIST. J Med Chem. Published online March 10, 2026. [Content Brief]

Calculators

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)}

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.

Bioz

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100 mg

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
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BLU-654

Alle PDGFR Isoform-spezifische Produkte anzeigen