ChemicalBook > CAS DataBase List > PD158780

PD158780

Product Name: PD158780
CAS No.: 171179-06-9
Chemical Name: PD158780
Synonyms: PD 158780 solution;PD 158780; PD-158780;InSolution? PD 158780;PD158780, 10 mM in DMSO;PD 158780 - CAS 171179-06-9 - Calbiochem;PD 158780, ErbB receptor tyrosine kinase inhibitor;InSolution PD 158780 - CAS 171179-06-9 - Calbiochem;N4-(3-Bromophenyl)-N6-methylpyrido[3,4-d]-4,6-pyrimidinediamine;N4-(3-Bromophenyl)-N6-methyl-pyrido[3,4-d]pyrimidine-4,6-diamine;Pyrido[3,4-d]pyriMidine-4,6-diaMine,N4-(3-broMophenyl)-N6-Methyl-
CBNumber: CB71074528
Molecular Formula: C14H12BrN5
Formula Weight: 330.18
MOL File: 171179-06-9.mol

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PD158780 Property

Melting point:: 174.0 to 178.0 °C
Boiling point:: 499.6±45.0 °C(Predicted)
Density: 1.611±0.06 g/cm3 (20 ºC 760 Torr)
storage temp.: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
solubility: DMSO: ≥20mg/mL
form: Yellow solid
pka: 5.80±0.30(Predicted)
color: yellow

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Safety

Hazard Codes: Xn
Risk Statements: 22
HS Code: 2912.49.2600

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P330Rinse mouth.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: 513035
Product name: PD 158780 - CAS 171179-06-9 - Calbiochem
Purity: A potent, cell-permeable, reversible, ATP-competitive inhibitor of the EGFR tyrosine kinase activity (IC?? = 8 pM).
Packaging: 500μg
Price: $189
Updated: 2025/07/31

Sigma-Aldrich

Product number: 513036
Product name: InSolution PD 158780 - CAS 171179-06-9 - Calbiochem
Packaging: 500μg
Price: $195
Updated: 2023/01/07

TCI Chemical

Product number: P2567
Product name: PD 158780
Purity: >97.0%(HPLC)
Packaging: 10mg
Price: $207
Updated: 2025/07/31

TCI Chemical

Product number: P2567
Product name: PD 158780
Purity: >97.0%(HPLC)
Packaging: 50mg
Price: $727
Updated: 2025/07/31

Cayman Chemical

Product number: 13329
Product name: PD 158780
Purity: ≥98%
Packaging: 1mg
Price: $37
Updated: 2024/03/01

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PD158780 Chemical Properties,Usage,Production

Uses

PD 158780 is a potent tyrosine kinase inhibitor of the epidermal growth factor receptor and has been shown to delay substantial growth of tumors in vivo tumor models.

Definition

ChEBI: PD158780 is a pyridopyrimidine that is pyrido[3,4-d]pyrimidine-4,6-diamine in which the amino groups at positions 4 and 6 are substituted by a m-bromophenyl group and a methyl group, respectively. It is a potent, cell-permeable, reversible ATP-competitive inhibitor of EGFR tyrosine kinase activity [IC50 values of 0.008, 49 and 52 nM for EGFR, ErbB2 (HER2) and Erb4 (HER4)]. It does not inhibit FGF or PDGF-mediated tyrosine phosphorylation. Induces G1 cell cycle arrest in MCF10A cells and is antiproliferative in A431 human epidermal carcinoma cells. It has a role as an antineoplastic agent and an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor. It is a pyridopyrimidine, a secondary amino compound, a member of bromobenzenes, a diamine and an aromatic amine.

General Description

A potent inhibitor of the EGFR tyrosine kinase activity (8 pM). Also inhibits heregulin-stimulated autophosphorylation in SK-BR-3 (IC₅₀ =49 nM) and MDA-MB-453 (IC₅₀ = 52 nM) breast carcinomas. The inhibition is competitive and results from binding of the inhibitor at the ATP site of the enzymes. Inhibits the LPA-stimulated MAP kinase kinase 1/2 (MKK1/2) activation and EGFR tyrosine phosphorylation in HeLa and NIH3T3 cells.

Biological Activity

Potent inhibitor of ErbB receptor family tyrosine kinases (IC 50 values are 0.008, 49 and 52 nM for EGFR, ErbB2 and ErbB2/ErbB4 respectively) that does not inhibit FGF or PDGF-mediated tyrosine phosphorylation. Induces G 1 cell cycle arrest in MCF10A cells and is antiproliferative in A431 human epidermal carcinoma cells.

Biochem/physiol Actions

Cell permeable: yes

Synthesis

171179-03-6

171179-06-9

Example 60: Synthesis of N4-(3-bromophenyl)-N6-methylpyrido[3,4-d]pyrimidine-4,6-diamine N-(3-Bromophenyl)-6-fluoro-pyrido[3,4-D]pyrimidin-4-amine (0.20 g, 0.63 mmol) was placed in a pressure vessel and an ethanol solution of methylamine was added and reacted at 100 °C. After completion of the reaction, purification was carried out by alumina column chromatography with the eluent dichloromethane/methanol (99:1, v/v) to afford the target product N4-(3-bromophenyl)-N6-methylpyrido[3,4-d]pyrimidine-4,6-diamine (0.07 g, 34% yield). 1H NMR (DMSO) δ 9.69 (1H, s), 8.75 (1H, s), 8.41 (1H, s), 8.21 (1H, brs), 7.93 (1H, brd, J = 7.6 Hz), 7.41-7.28 (2H, m), 7.06 (1H, s), 6.82 (1H, q, J = 5.0 Hz), 4.95 ( 3H, d, J = 5.0 Hz).

storage

Store at -20°C

References

[1] Patent: US5654307, 1997, A

PD158780 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from PD158780 manufacturers

Career Henan Chemical Co

Product: PD158780 171179-06-9
Price: US $1.00/KG
Min. Order: 1KG
Purity: 98%
Supply Ability: 200kgs
Release date: 2020-01-28

171179-06-9, PD158780Related Search:

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N4-(3-Bromophenyl)-N6-methyl-pyrido[3,4-d]pyrimidine-4,6-diamine

Pyrido[3,4-d]pyriMidine-4,6-diaMine,N4-(3-broMophenyl)-N6-Methyl- (Related Reference)

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PD 158780 solution

InSolution? PD 158780

PD 158780 - CAS 171179-06-9 - Calbiochem

InSolution PD 158780 - CAS 171179-06-9 - Calbiochem

PD 158780; PD-158780

PD158780,Inhibitor,Epidermal growth factor receptor,inhibit,HER1,EGFR,PD 158780,ErbB-1,PD-158780

PD 158780, ErbB receptor tyrosine kinase inhibitor

PD158780, 10 mM in DMSO

N4-(3-Bromophenyl)-N6-methylpyrido[3,4-d]-4,6-pyrimidinediamine

171179-06-9