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PD0166285 - ≥99%, high purity , CAS No.185039-89-8, Inhibitor of epidermal growth factor receptor;Inhibitor of fibroblast growth factor receptor 1;Inhibitor of platelet derived growth factor receptor beta;Inhibitor of protein kinase; membrane associated tyrosine/threonine 1;Inhibitor of SRC proto-oncogene;

  • Moligand™
  • ≥99%
Item Number
P276244
Grouped product items
SKUSizeAvailabilityPrice Qty
P276244-1mg
1mg
In stock
$39.90
P276244-5mg
5mg
In stock
$162.90
P276244-10mg
10mg
In stock
$260.90
P276244-25mg
25mg
In stock
$587.90
P276244-50mg
50mg
In stock
$1,022.90

Inhibitors of SRC/FGFR1/PDGFR β/Wee1

Basic Description

SynonymsPD0166285|185039-89-8|PD166285|PD-166285|TCMDC-140940|CHEMBL49120|6-(2,6-dichlorophenyl)-2-[4-[2-(diethylamino)ethoxy]anilino]-8-methylpyrido[2,3-d]pyrimidin-7-one|PD-0166285|6-(2,6-dichlorophenyl)-2-((4-(2-(diethylamino)ethoxy)phenyl)amino)-8-methylpyrid
Specifications & PurityMoligand™, ≥99%
Biochemical and Physiological MechanismsPD0166285 is a substrate of P-GP, and is an inhibitor of WEE1. It can also weakly inhibit Myt1, with IC50 values of 24 and 72 nM, respectively. PD0166285 has an IC50 value of 3.433 μm against CHK1.
Storage TempStore at -20°C,Desiccated
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of epidermal growth factor receptor;Inhibitor of fibroblast growth factor receptor 1;Inhibitor of platelet derived growth factor receptor beta;Inhibitor of protein kinase; membrane associated tyrosine/threonine 1;Inhibitor of SRC proto-oncogene;
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

Store at -20°C. Store under desiccating conditions.

Associated Targets

CDK1 Tchem Cyclin-dependent kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK7 Tchem Cyclin-dependent kinase 7 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DYRK1B Tchem Dual specificity tyrosine-phosphorylation-regulated kinase 1B 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DYRK1A Tchem Dual specificity tyrosine-phosphorylation-regulated kinase 1A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

EGFR Tclin Epidermal growth factor receptor 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CSF1R Tclin Macrophage colony-stimulating factor 1 receptor 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK9 Tchem Cyclin-dependent kinase 9 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK5 Tchem Cyclin-dependent-like kinase 5 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

RET Tclin Proto-oncogene tyrosine-protein kinase receptor Ret 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SRC Tclin Proto-oncogene tyrosine-protein kinase Src 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ROCK2 Tclin Rho-associated protein kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MST1R Tchem Macrophage-stimulating protein receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ROCK1 Tclin Rho-associated protein kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

STK17A Tchem Serine/threonine-protein kinase 17A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

YES1 Tclin Tyrosine-protein kinase Yes 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FGFR1 Tclin Fibroblast growth factor receptor 1 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MET Tclin Hepatocyte growth factor receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

IGF1R Tclin Insulin-like growth factor 1 receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

JAK3 Tclin Tyrosine-protein kinase JAK3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TAOK1 Tchem Serine/threonine-protein kinase TAO1 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PIM1 Tchem Serine/threonine-protein kinase pim-1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PDGFRA Tclin Platelet-derived growth factor receptor alpha 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PDGFRB Tclin Platelet-derived growth factor receptor beta 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAP2K2 Tclin Dual specificity mitogen-activated protein kinase kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAP4K5 Tchem Mitogen-activated protein kinase kinase kinase kinase 5 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BTK Tclin Tyrosine-protein kinase BTK 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKA Tchem Aurora kinase A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKB Tchem Aurora kinase B 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FLT1 Tclin Vascular endothelial growth factor receptor 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

KDR Tclin Vascular endothelial growth factor receptor 2 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TNK2 Tclin Activated CDC42 kinase 1 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ALK Tclin ALK tyrosine kinase receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CHEK1 Tchem Serine/threonine-protein kinase Chk1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CLK2 Tchem Dual specificity protein kinase CLK2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CLK4 Tchem Dual specificity protein kinase CLK4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GSK3A Tclin Glycogen synthase kinase-3 alpha 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SLC2A1 Tchem Solute carrier family 2, facilitated glucose transporter member 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

NTRK1 Tclin High affinity nerve growth factor receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

JAK2 Tclin Tyrosine-protein kinase JAK2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PRKACA Tchem cAMP-dependent protein kinase catalytic subunit alpha 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PRKCQ Tchem Protein kinase C theta type 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAP2K1 Tclin Dual specificity mitogen-activated protein kinase kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 6-(2,6-dichlorophenyl)-2-[4-[2-(diethylamino)ethoxy]anilino]-8-methylpyrido[2,3-d]pyrimidin-7-one
INCHI InChI=1S/C26H27Cl2N5O2/c1-4-33(5-2)13-14-35-19-11-9-18(10-12-19)30-26-29-16-17-15-20(25(34)32(3)24(17)31-26)23-21(27)7-6-8-22(23)28/h6-12,15-16H,4-5,13-14H2,1-3H3,(H,29,30,31)
InChi Key IFPPYSWJNWHOLQ-UHFFFAOYSA-N
Canonical SMILES CCN(CC)CCOC1=CC=C(C=C1)NC2=NC=C3C=C(C(=O)N(C3=N2)C)C4=C(C=CC=C4Cl)Cl
Isomeric SMILES CCN(CC)CCOC1=CC=C(C=C1)NC2=NC=C3C=C(C(=O)N(C3=N2)C)C4=C(C=CC=C4Cl)Cl
PubChem CID 5311382
Molecular Weight 512.43

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

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5 results found

Lot NumberCertificate TypeDateItem
B2224647Certificate of AnalysisDec 12, 2022 P276244
B2225076Certificate of AnalysisDec 12, 2022 P276244
B2225084Certificate of AnalysisDec 12, 2022 P276244
B2225090Certificate of AnalysisDec 12, 2022 P276244
B2224381Certificate of AnalysisDec 12, 2022 P276244

Chemical and Physical Properties

SolubilitySoluble in DMSO to 100 mM and in ethanol to 100 mM

Safety and Hazards(GHS)

Pictogram(s) GHS07
Signal Warning
Hazard Statements

H315:Causes skin irritation

H319:Causes serious eye irritation

H335:May cause respiratory irritation

H302:Harmful if swallowed

Precautionary Statements

P261:Avoid breathing dust/fume/gas/mist/vapors/spray.

P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing.

Related Documents

References

1. Wang Y, Li J, Booher RN, Kraker A, Lawrence T, Leopold WR, Sun Y.  (2001)  Radiosensitization of p53 mutant cells by PD0166285, a novel G(2) checkpoint abrogator..  Cancer Res,  61  (22): (8211-7).  [PMID:11719452]
2. Rohe A, Erdmann F, Bäßler C, Wichapong K, Sippl W, Schmidt M.  (2012)  In vitro and in silico studies on substrate recognition and acceptance of human PKMYT1, a Cdk1 inhibitory kinase..  Bioorg Med Chem Lett,  22  (2): (1219-23).  [PMID:22189141]
3. Panek RL, Lu GH, Klutchko SR, Batley BL, Dahring TK, Hamby JM, Hallak H, Doherty AM, Keiser JA.  (1997)  In vitro pharmacological characterization of PD 166285, a new nanomolar potent and broadly active protein tyrosine kinase inhibitor..  J Pharmacol Exp Ther,  283  (3): (1433-44).  [PMID:9400019]
4. Trumpp-Kallmeyer S, Rubin JR, Humblet C, Hamby JM, Showalter HD.  (1998)  Development of a binding model to protein tyrosine kinases for substituted pyrido[2,3-d]pyrimidine inhibitors..  J Med Chem,  41  (11): (1752-63).  [PMID:9599227]
5. Klutchko SR, Hamby JM, Boschelli DH, Wu Z, Kraker AJ, Amar AM, Hartl BG, Shen C, Klohs WD, Steinkampf RW et al..  (1998)  2-Substituted aminopyrido[2,3-d]pyrimidin-7(8H)-ones. structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity..  J Med Chem,  41  (17): (3276-92).  [PMID:9703473]

Solution Calculators