Cat. No.: HY-112301A

trans-Pralsetinib

(Synonyms: trans-BLU-667)

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trans-Pralsetinib (trans-BLU-667) is a rearranged during transfection (RET) inhibitor extracted from patent US20170121312A1, Compound Example 129.

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Pureté: 98.06%
CAS No.: 2097132-93-7
Formule: C₂₇H₃₂FN₉O₂
Masse moléculaire:533.60

Stockage:

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

trans-Pralsetinib Chemical Structure

CAS No.: 2097132-93-7

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

trans-Pralsetinib (trans-BLU-667) is a rearranged during transfection (RET) inhibitor extracted from patent US20170121312A1, Compound Example 129^[1].

IC₅₀ & Target

RET^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	1.266 μM Compound: BLU-667	Cytotoxicity against mouse BaF3 cells assessed as reduction in cell proliferation measured after 48 hrs by MTS assay Cytotoxicity against mouse BaF3 cells assessed as reduction in cell proliferation measured after 48 hrs by MTS assay	[PMID: 32882611]
BaF3	IC₅₀	>261 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase G810C-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase G810C-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	1040 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells incubated for 72 hrs by CCK8 assay	[PMID: 36905915]
BaF3	IC₅₀	114 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells expressing CCDC6-RET-G810C incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing CCDC6-RET-G810C incubated for 72 hrs by CCK8 assay	[PMID: 36905915]
BaF3	IC₅₀	1170 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	17 nM Compound: BLU-667	Antiproliferative activity against mouse KIF5B-RET BaF3 cells by cell based assay Antiproliferative activity against mouse KIF5B-RET BaF3 cells by cell based assay	[PMID: 34058344]
BaF3	IC₅₀	21.7 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-G810S incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-G810S incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	215 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-G810C incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-G810C incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	241 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-G810R incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-G810R incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	3.5 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804M-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804M-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	358 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells expressing CCDC6-RET-G810R incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing CCDC6-RET-G810R incubated for 72 hrs by CCK8 assay	[PMID: 36905915]
BaF3	IC₅₀	4.1 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-KIF5B incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-KIF5B incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	4.1 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells expressing CCDC6-RET-V804M incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing CCDC6-RET-V804M incubated for 72 hrs by CCK8 assay	[PMID: 36905915]
BaF3	IC₅₀	4.4 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells expressing wildtype rearranged during transfection kinase-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing wildtype rearranged during transfection kinase-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	5 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells expressing CCDC6-RET incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing CCDC6-RET incubated for 72 hrs by CCK8 assay	[PMID: 36905915]
BaF3	IC₅₀	5.7 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells expressing wildtype rearranged during transfection kinase-KIF5B incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing wildtype rearranged during transfection kinase-KIF5B incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	575 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase G810R-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase G810R-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	9.2 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804M-KIF5B incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804M-KIF5B incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]

Chemical Information

CAS No. 2097132-93-7
Appearance Solid
Masse moléculaire 533.60
Formule C₂₇H₃₂FN₉O₂
Color Light yellow to yellow
SMILES

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

trans-BLU-667
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (187.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

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. 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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: ≥ 4.55 mg/mL (8.53 mM); Clear solution

This protocol yields a clear solution of ≥ 4.55 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.5 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% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.69 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (268 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 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)
Instruction de manipulation (2659 KB)

Références

[1]. Jason D. Brubaker, et al. Inhibitors of ret. US20170121312A1.

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8741 mL	9.3703 mL	18.7406 mL	46.8516 mL
	5 mM	0.3748 mL	1.8741 mL	3.7481 mL	9.3703 mL
	10 mM	0.1874 mL	0.9370 mL	1.8741 mL	4.6852 mL
	15 mM	0.1249 mL	0.6247 mL	1.2494 mL	3.1234 mL
	20 mM	0.0937 mL	0.4685 mL	0.9370 mL	2.3426 mL
	25 mM	0.0750 mL	0.3748 mL	0.7496 mL	1.8741 mL
	30 mM	0.0625 mL	0.3123 mL	0.6247 mL	1.5617 mL
	40 mM	0.0469 mL	0.2343 mL	0.4685 mL	1.1713 mL
	50 mM	0.0375 mL	0.1874 mL	0.3748 mL	0.9370 mL
	60 mM	0.0312 mL	0.1562 mL	0.3123 mL	0.7809 mL
	80 mM	0.0234 mL	0.1171 mL	0.2343 mL	0.5856 mL
	100 mM	0.0187 mL	0.0937 mL	0.1874 mL	0.4685 mL

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trans-Pralsetinib

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Anti-Lung Cancer Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Human Metabolite Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

trans-Pralsetinib

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Anti-Lung Cancer Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Human Metabolite Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

trans-Pralsetinib Related Classifications

HY-112301A Related Classifications