1. Protein Tyrosine Kinase/RTK
  2. RET
  3. Pralsetinib

Pralsetinib (Synonyms: Blu667)

Cat. No.: HY-112301 Purity: 99.56%
Handling Instructions

Pralsetinib (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.

Pralsetinib Chemical Structure

Pralsetinib Chemical Structure

CAS No. : 2097132-94-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 188 In-stock
Estimated Time of Arrival: December 31
5 mg USD 160 In-stock
Estimated Time of Arrival: December 31
10 mg USD 250 In-stock
Estimated Time of Arrival: December 31
50 mg USD 750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1250 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Pralsetinib:

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target

IC50: 0.4 nM (Wild type RET)[1]

In Vitro

Pralsetinib (Blu667) demonstrates more than 10-fold increased potency over approved MKIs against oncogenic RET variants and resistance mutants[1].
Pralsetinib (Blu667) 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[1].
Pralsetinib (Blu667) 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)[1].

In Vivo

Pralsetinib (Blu667) 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)[1].
Pralsetinib (Blu667) shows 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[1].

Clinical Trial
Molecular Weight

533.60

Formula

C₂₇H₃₂FN₉O₂

CAS No.

2097132-94-8

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (187.41 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.69 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.69 mM); Clear solution

*All of the co-solvents are provided by MCE.
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 Pralsetinib (Blu667) or once-daily with 60 mg/kg Pralsetinib (Blu667) or 60 mg/kg XL184[2].

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

References

Purity: 99.56%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Pralsetinib
Cat. No.:
HY-112301
Quantity: