2. Protein Tyrosine Kinase/RTK
  3. c-Kit PDGFR
  4. 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 KITV654A over most other kinases in the kinome. BLU-654 exerts sustained antineoplastic activity in KITV654A cell-derived xenograft mouse models. BLU-654 can be used in research related to Imatinib (HY-15463)-resistant gastrointestinal stromal tumors.

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

BLU-654

BLU-654 Chemical Structure

CAS No. : 2999638-62-7

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Description

BLU-654 is an orally active antineoplastic agent and KIT inhibitor. BLU-654 is a highly selective inhibitor targeting wild-type KIT, PDGFRβ, and KITV654A over most other kinases in the kinome. BLU-654 exerts sustained antineoplastic activity in KITV654A cell-derived xenograft mouse models. BLU-654 can be used in research related to Imatinib (HY-15463)-resistant gastrointestinal stromal tumors[1].

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 KITV654A 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 KITV654A 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.

BLU-654 Related Antibodies
Parmacokinetics
Species Dose Route CLplasma T1/2 Vss 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.
Molecular Weight

429.49

Formula

C21H28FN7O2
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BLU-654 Related Classifications

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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.

Keywords:

BLU-6542999638-62-7BLU654BLU 654c-KitPDGFRSCFRCD117Platelet-derived growth factor receptorHMC1.1 11/13 cellsxenograft mouse modelsPDGFRβkinome kinasesCaco-2 cellsKIT V654Awild-type KITSW569 cellsgastrointestinal stromal tumorM-07e cellsInhibitorinhibitorinhibit

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