Art. -Nr.: HY-155537

Pruvonertinib

(Synonyms: YK-029A)

1 Cited Publications

Kundenbewertung

Based on 1 publication(s) in Google Scholar

YK-029A is an orally active inhibitor of mutant EGFR，targeting to both the T790M mutations (EGFR^T790M) and exon 20 insertion of EGFR (EGFRex20ins). YK-029A exhibits significant antitumor activity，and results tumor regression in EGFRex20ins-driven PDX models.

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Reinheit: 99.50%
CAS. Nr.: 2064269-82-3
Formel: C₂₇H₃₂N₈O₂
Molecular Weight:500.60

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Pruvonertinib Chemical Structure

CAS. Nr.: 2064269-82-3

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Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

EGFR^T790M, EGFRex20ins^[1]

Alle EGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	GI₅₀	267 nM Compound: 6; YK-029A	Antiproliferative activity against human A-431 cells harboring wildtype EGFR assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against human A-431 cells harboring wildtype EGFR assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay	[PMID: 37406381]
BaF3	GI₅₀	3.4 nM Compound: 6; YK-029A	Antiproliferative activity against mouse BaF3 cells harboring EGFR A763_Y764ins_FQEA mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells harboring EGFR A763_Y764ins_FQEA mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay	[PMID: 37406381]
BaF3	GI₅₀	35 nM Compound: 6; YK-029A	Antiproliferative activity against mouse BaF3 cells harboring EGFR D770_N771ins_SVD mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells harboring EGFR D770_N771ins_SVD mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay	[PMID: 37406381]
BaF3	GI₅₀	69 nM Compound: 6; YK-029A	Antiproliferative activity against mouse BaF3 cells harboring EGFR H773_V774ins_NPH mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells harboring EGFR H773_V774ins_NPH mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay	[PMID: 37406381]
BaF3	GI₅₀	70 nM Compound: 6; YK-029A	Antiproliferative activity against mouse BaF3 cells harboring EGFR V769_D770ins_ASV mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells harboring EGFR V769_D770ins_ASV mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay	[PMID: 37406381]
HCC827	GI₅₀	3.4 nM Compound: 6; YK-029A	Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay	[PMID: 37406381]
NCI-H1975	GI₅₀	12 nM Compound: 6; YK-029A	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay	[PMID: 37406381]
PC-9	GI₅₀	7.2 nM Compound: 6; YK-029A	Antiproliferative activity against human PC-9 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against human PC-9 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay	[PMID: 37406381]

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2064269-82-3
Appearance Solid
Molecular Weight 500.60
Formel C₂₇H₃₂N₈O₂
Color Off-white to light yellow
SMILES

C=CC(NC1=CC(NC2=NC=CC(C3=CN=C4C(C)=CC=CN43)=N2)=C(OC)C=C1N(CCN(C)C)C)=O
Synonyms

YK-029A
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Journal Impact Factor

J Med Chem

Profiling and Optimizing Targeted Covalent Inhibitors through EGFR-Guided Studies. [Abstract]

2025 Aug 28;68(16):17917-17932. PMID: 40801664

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (199.76 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

1.9976 mL

9.9880 mL

19.9760 mL

5 mM

0.3995 mL

1.9976 mL

3.9952 mL

10 mM

0.1998 mL

0.9988 mL

1.9976 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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)}

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: 2.5 mg/mL (4.99 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 (4.99 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)
Handling Instructions (2659 KB)

Verweise

[1]. Liu B, et al. Discovery of YK-029A, a novel mutant EGFR inhibitor targeting both T790 M and exon 20 insertion mutations, as a treatment for NSCLC. Eur J Med Chem. 2023 Oct 5;258:115590. [Content Brief]

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9976 mL	9.9880 mL	19.9760 mL	49.9401 mL
	5 mM	0.3995 mL	1.9976 mL	3.9952 mL	9.9880 mL
	10 mM	0.1998 mL	0.9988 mL	1.9976 mL	4.9940 mL
	15 mM	0.1332 mL	0.6659 mL	1.3317 mL	3.3293 mL
	20 mM	0.0999 mL	0.4994 mL	0.9988 mL	2.4970 mL
	25 mM	0.0799 mL	0.3995 mL	0.7990 mL	1.9976 mL
	30 mM	0.0666 mL	0.3329 mL	0.6659 mL	1.6647 mL
	40 mM	0.0499 mL	0.2497 mL	0.4994 mL	1.2485 mL
	50 mM	0.0400 mL	0.1998 mL	0.3995 mL	0.9988 mL
	60 mM	0.0333 mL	0.1665 mL	0.3329 mL	0.8323 mL
	80 mM	0.0250 mL	0.1249 mL	0.2497 mL	0.6243 mL
	100 mM	0.0200 mL	0.0999 mL	0.1998 mL	0.4994 mL

Keywords

Pruvonertinib

1 Cited Publications

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Pruvonertinib

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) Pruvonertinib

Alle EGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Pruvonertinib

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) Pruvonertinib

Alle EGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Pruvonertinib Related Classifications

HY-155537 Related Classifications