Cat. No.: HY-112411

PD 174265

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PD 174265 is a highly selective, reversible EGFR/ErbB2 tyrosine kinase inhibitor (IC₅₀=0.45 nM) and cell differentiation inducer. By blocking receptor autophosphorylation and the downstream ERK signaling pathway (with an IC₅₀ of 0.45 μM for full-length ERK), PD 174265 effectively inhibits tumor growth and exhibits antitumor activity without obvious toxicity in in vivo models. PD 174265 drives oligodendrocyte precursor cells to switch from a proliferative state to a differentiated state, significantly upregulates the expression of myelin proteins such as CNP, PLP and MBP, and induces neurite branching. PD 174265 shows no inhibitory effect on other kinases including insulin, PDGF and basic FGF receptors, and serves as a crucial tool molecule for investigating the treatment of human epidermoid carcinoma and the mechanism of myelin repair in multiple sclerosis.

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

Purity: 98.35%
CAS No.: 216163-53-0
Formula: C₁₇H₁₅BrN₄O
Molecular Weight:371.23

Storage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

PD 174265 Chemical Structure

CAS No.: 216163-53-0

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

ErbB2

All EGFR Isoforms :

All ERK Isoforms :

All PDGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	GI₅₀	0.021 μM Compound: PD-168393	Growth inhibition of human A431 cells after 72 hrs by MTT assay Growth inhibition of human A431 cells after 72 hrs by MTT assay	[PMID: 19969465]
BaF3	GI₅₀	<0.5 μM Compound: 3d	Growth inhibition of mouse BA/F3 cells expressing EGFR Del1 mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR Del1 mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
BaF3	GI₅₀	<0.5 μM Compound: 3d	Growth inhibition of mouse BA/F3 cells expressing EGFR Del3 mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR Del3 mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
BaF3	GI₅₀	<0.5 μM Compound: 3d	Growth inhibition of mouse BA/F3 cells expressing EGFR Del5 mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR Del5 mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
BaF3	GI₅₀	<0.5 μM Compound: 3d	Growth inhibition of mouse BA/F3 cells expressing EGFR L858R mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR L858R mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
BaF3	GI₅₀	>0.5 μM Compound: 3d	Growth inhibition of mouse BA/F3 cells expressing EGFR Del3 and Thr790Met mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR Del3 and Thr790Met mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
BaF3	GI₅₀	>5 μM Compound: 3d	Growth inhibition of mouse BA/F3 cells expressing EGFR Del1 and Thr790Met mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR Del1 and Thr790Met mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
BaF3	GI₅₀	>5 μM Compound: 3d	Growth inhibition of mouse BA/F3 cells expressing EGFR Del5 and Thr790Met mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR Del5 and Thr790Met mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
BaF3	GI₅₀	>5 μM Compound: 3d	Growth inhibition of mouse BA/F3 cells expressing EGFR L858R and Thr790Met mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR L858R and Thr790Met mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]

In Vitro

PD 174265 (1-10 μM; 72 h, 3 days) induces the differentiation of Oli-neu mouse oligodendrocyte precursor cells, which is characterized by increased axonal growth and upregulated expression of myelin-related markers CNP, PLP and MBP; specifically, when treated with 1 μM for 72 h, the induced expression level of MBP mRNA reaches approximately 8 times that of the control group, representing the maximum value^[1].
PD 174265 (1 μM; 3 d) induces differentiation of primary rat oligodendrocyte precursor cells, as evidenced by increased mRNA and protein levels of myelin markers CNP, MBP and PLP following 3 days of treatment with 1 μM^[1].
PD 174265 (2 μM; 1 h) reversibly inhibits EGF-dependent EGFr autophosphorylation in A431 human epidermoid carcinoma cells, and the activity recovers completely after 8 hr of culture in medium without this compound^[2].
PD 174265 reversibly inhibits EGF-induced EGFR autophosphorylation in A431 human epidermal cancer cells (IC₅₀=39 nM), as well as heregulin-induced erbB2 autophosphorylation in MDA-MB-453 human breast cancer cells (IC₅₀=220 nM)^[2].
PD 174265 (following 4 h of EGF/TGF pretreatment and under variable co-incubation conditions) reverses the EGF- and TGF-induced increase in PS-ASO activity in A431 cells by blocking the phosphorylation of EGFR and ERK, restoring the IC₅₀ value of PS-ASO to the level of the control group^[3].
PD 174265 (1 μM; 10 min preincubation) causes a non-specific false-positive increase in mitochondrial ROS production in adult rabbit ventricular myocytes, with a level comparable to that induced by acetylcholine^[4].

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

Cell Differentiation Assay^[1]

Cell Line:

Oli-neu mouse oligodendrocyte precursor cell
Concentration:

1-10 μM (screening); 1 μM (morphological analysis and Western blotting); serial dilutions (dose-response curve)
Incubation Time:

72 h (screening); 3 days (morphological analysis, Western blotting, dose-response curve)
Result:

Induced dose-dependent Oli-neu differentiation, with extensive cellular branching at optimal concentrations. Stimulated time-dependent upregulation of CNP, PLP, and MBP mRNA: by 72 h, MBP mRNA reached ~8-fold over control, CNP mRNA reached ~4-fold over control, and PLP mRNA reached ~4-fold over control. Induced time-dependent increases in CNP and MBP protein, with peak expression at 3 days of treatment. Produced a sigmoidal dose-response curve for the neurite outgrowth index, with activity increasing at concentrations above 0.1 μM.

In Vivo

PD 174265 (58 mg/kg; i.p.; on days 10-14, 17-21, and 24-28 after tumor implant) exhibits weak in vivo antitumor activity against A431 human epidermoid carcinoma xenografts in nude mice, with 13% tumor growth inhibition, and only transiently suppresses EGFR phosphotyrosine content^[2].

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

Animal Model:

Athymic nude mice with Epidermoid carcinoma^[2]
Dosage:

58 mg/kg (antitumor activity); 58 mg/kg (EGFr phosphotyrosine analysis)
Administration:

i.p.; on days 10-14, 17-21, and 24-28 after tumor implant (antitumor activity); single dose (EGFr phosphotyrosine analysis)
Result:

Produced a tumor growth inhibition of 13%. Reduced EGFr phosphotyrosine content by ~80% at 4 hours post-injection. Returned EGFr phosphotyrosine content to ~75% of control levels by 8 hours post-injection. Restored EGFr phosphotyrosine content to 100% of control levels by 24 hours post-injection.

Chemical Information

CAS No. 216163-53-0
Appearance Solid
Molecular Weight 371.23
Formula C₁₇H₁₅BrN₄O
Color Light yellow to yellow
SMILES

CCC(NC1=CC2=C(NC3=CC=CC(Br)=C3)N=CN=C2C=C1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (336.72 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

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6937 mL

13.4687 mL

26.9375 mL

5 mM

0.5387 mL

2.6937 mL

5.3875 mL

10 mM

0.2694 mL

1.3469 mL

2.6937 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)

References

[1]. Joubert L, et al. Chemical inducers and transcriptional markers of oligodendrocyte differentiation. J Neurosci Res. 2010;88(12):2546-2557. [Content Brief]

[2]. Fry DW, et al. Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor. Proc Natl Acad Sci U S A. 1998;95(20):12022-12027. [Content Brief]

[3]. Wang S, et al. Cellular uptake mediated by epidermal growth factor receptor facilitates the intracellular activity of phosphorothioate-modified antisense oligonucleotides. Nucleic Acids Res. 2018;46(7):3579-3594. [Content Brief]

[4]. Krieg T, et al. Mitochondrial ROS generation following acetylcholine-induced EGF receptor transactivation requires metalloproteinase cleavage of proHB-EGF. J Mol Cell Cardiol. 2004;36(3):435-443. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6937 mL	13.4687 mL	26.9375 mL	67.3437 mL
	5 mM	0.5387 mL	2.6937 mL	5.3875 mL	13.4687 mL
	10 mM	0.2694 mL	1.3469 mL	2.6937 mL	6.7344 mL
	15 mM	0.1796 mL	0.8979 mL	1.7958 mL	4.4896 mL
	20 mM	0.1347 mL	0.6734 mL	1.3469 mL	3.3672 mL
	25 mM	0.1077 mL	0.5387 mL	1.0775 mL	2.6937 mL
	30 mM	0.0898 mL	0.4490 mL	0.8979 mL	2.2448 mL
	40 mM	0.0673 mL	0.3367 mL	0.6734 mL	1.6836 mL
	50 mM	0.0539 mL	0.2694 mL	0.5387 mL	1.3469 mL
	60 mM	0.0449 mL	0.2245 mL	0.4490 mL	1.1224 mL
	80 mM	0.0337 mL	0.1684 mL	0.3367 mL	0.8418 mL
	100 mM	0.0269 mL	0.1347 mL	0.2694 mL	0.6734 mL

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PD 174265

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glutamine Metabolism Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

All EGFR Isoforms

All ERK Isoforms

All PDGFR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PD 174265 Related Classifications

Cat. No.: HY-112411