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Blu667 

Cat. No.: HY-112301
Handling Instructions

Blu667 is a highly potent and selective RET inhibitor with an IC50 of 0.4 nM for wild type RET kinase.

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

Blu667 Chemical Structure

Blu667 Chemical Structure

CAS No. : 2097132-94-8

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Blu667 is a highly potent and selective RET inhibitor with an IC50 of 0.4 nM for wild type RET kinase.

IC50 & Target

IC50: 0.12 nM (Wild type RET)[2]

In Vitro

Blu667 is a RET inhibitor extracted from patent US20170121312A1, compound example 129[1]. BLU-667 demonstrates more than 10-fold increased potency over approved MKIs against oncogenic RET variants and resistance mutants. BLU-667 demonstrates potent activity (IC50=0.4 nM) against common oncogenic RET alterations, including RET M918T, an activating mutation found in MTC, as well as the CCDC6-RET fusion observed in PTC and NSCLC. BLU-667 suppresses RET pathway signaling in a panel of RET-driven cell lines: LC2/ad (CCDC6-RET, NSCLC), MZ-CRC-1 (RET M918T, MTC), and TT (RET C634W, MTC)[2].

In Vivo

BLU-667 potently inhibits growth of NSCLC and thyroid cancer xenografts driven by various RET mutations and fusions without inhibiting vascular endothelial growth factor receptor 2 (VEGFR-2). BLU667 showed potent dose dependent activity against both KIF5B-RET Ba/F3 and KIF5B-RET V804L Ba/F3 allograft tumors with doses as low as 10 mg/kg twice-daily[2].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8741 mL 9.3703 mL 18.7406 mL
5 mM 0.3748 mL 1.8741 mL 3.7481 mL
10 mM 0.1874 mL 0.9370 mL 1.8741 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

KIF5B-RET Ba/F3 cells are exposed to compound concentrations ranging from 25 µM to 95.4 pM for 48 hours, and proliferation is assessed with Cell Titer Glo. TT, MZ-CRC-1, TPC-1 or LC2/ad cells are exposed to compound for 4 days and proliferation is measured by BrdU incorporation[2].

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

Animal Administration
[2]

Mice[2]

BALB/c nude mice are inoculated subcutaneously into the right flank with KIF5B-RET Ba/F3 cells, KIF5B-RET V804L Ba/F3 cells, or TT cells. For all experiments, mice are dosed twice-daily with vehicle, 3 mg/kg, 10 mg/kg, or 30 mg/kg BLU-667 or once-daily with 60 mg/kg BLU-667 or 60 mg/kg cabozantinib[2].

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

References
Molecular Weight

533.60

Formula

C₂₇H₃₂FN₉O₂

CAS No.

2097132-94-8

SMILES

O=C([[email protected]@]1(OC)CC[[email protected]@H](C2=NC(NC3=NNC(C)=C3)=CC(C)=N2)CC1)N[[email protected]](C4=CC=C(N5N=CC(F)=C5)N=C4)C

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Blu667
Cat. No.:
HY-112301
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Blu667

Cat. No.: HY-112301