Determine the necessary mass, volume, or concentration for preparing a solution.
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SKU | Size | Availability | Price | Qty |
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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
Synonyms | AKOS022190406 | SCHEMBL133914 | Kinome_3263 | BCP20228 | EX-A4179 | 6-(2,6-Dichloro-phenyl)-2-[4-(2-diethylamino-ethoxy)-phenylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one | 6-(2,6-Dichlorophenyl)-2-[4-(2-diethylaminoethoxy)-phenylamino]-8-methyl-8H-py |
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Specifications & Purity | Moligand™, ≥99% |
Biochemical and Physiological Mechanisms | PD0166285 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 Temp | Store at -20°C,Desiccated |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | 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; |
Note | Wherever 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. |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 6-(2,6-dichlorophenyl)-2-[4-[2-(diethylamino)ethoxy]anilino]-8-methylpyrido[2,3-d]pyrimidin-7-one |
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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 |
PubChem CID | 5311382 |
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ChEMBL Ligand | CHEMBL49120 |
CAS Registry No. | 185039-89-8 |
BindingDB Ligand | 3096 |
RCSB PDB Ligand | 96M |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
---|---|---|---|
B2224647 | Certificate of Analysis | Dec 12, 2022 | P276244 |
B2225076 | Certificate of Analysis | Dec 12, 2022 | P276244 |
B2225084 | Certificate of Analysis | Dec 12, 2022 | P276244 |
B2225090 | Certificate of Analysis | Dec 12, 2022 | P276244 |
B2224381 | Certificate of Analysis | Dec 12, 2022 | P276244 |
Solubility | Soluble in DMSO to 100 mM and in ethanol to 100 mM |
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Pictogram(s) | GHS07 |
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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. |
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] [10.1021/op500134e] |
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] [10.1021/op500134e] |
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] [10.1021/op500134e] |
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] [10.1021/op500134e] |
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] [10.1021/op500134e] |