PD 166285
Synonym(s):PD 166285 - CAS 212391-63-4 - Calbiochem;PD166285, PD0166285, 6-(2,6-Dichlorophenyl)-2-(4-(2-(diethylaminoethoxy)-phenylamino)-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one, 2HCl, PDGFR Tyrosine Kinase Inhibitor XIX, Wee1 Inhibitor IV;PDGFR Tyrosine Kinase Inhibitor XIX, Wee1 Inhibitor IV, 6-(2,6-Dichlorophenyl)-2-(4-(2-(diethylaminoethoxy)-phenylamino)-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one, 2HCl, PD166285, PD0166285
- CAS NO.:212391-63-4
- Empirical Formula: C26H29Cl4N5O2
- Molecular Weight: 585.37
- MDL number: MFCD18086890
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-30 15:45:59
What is PD 166285?
Chemical properties
Yellow Solid
The Uses of PD 166285
A broad-spectrum receptor tyrosine kinase (RTK) inhibitor which shows anti-angiogenic activity and anti-tumor efficacy in combination with photodynamic therapy (PDT).
What are the applications of Application
PD 166285 is an inhibitor of RTK, c-Src, FGFR1, Wee 1, and PDGFRβ
General Description
A cell-permeable, orally bioavailable, ATP-competitive, broad-spectrum tyrosine kinase inhibitor (IC50 against against c-Src, Wee1, FGFR-1, Myt1, EGFR, and PDGFRβ = 8.4, 24, 39.3, 72, 87.5 and 98.3 nM, respectively) that suppresses angiogenesis both in vitro (max inhibition dose at 100 nM in HUVEC microcapillary formation assays) and in vivo (max inhibition achieved via 5 mg/kg p.o. in murine Matrigel plug angiogenesis assays), while exhibiting much reduced potency against Chk1, MAPK, and PKC (IC50 = 3.4, 5, and 22.7 μM, respectively) and little activity toward IRTK and Cdk4/D1 even at concentrations as high as 50 μM. Shown to effectively block PDGF-, EGF-, and bFGF-stimulated receptor phosphorylations (IC50 = 6.5, 1600, and 97.3 nM, respectively) and other cellular responses in rat aortic smooth muscle cells. Inhibition of cellular Wee1 activity by 500 nM PD 166285 in combination with 50 ng/ml nocodazole (Cat. No. 487928) treatment is also reported to result in a blockage of radiation-induced Cdc2 phosphorylation on Tyr15 and Thr14 in 7 human cancer cells and specifically demonstrated to sensatize PA-1 cultures to radiation-induced cell death in a p53-dependent manner.
Biological Activity
Potent inhibitor of the tyrosine kinases c-Src, fibroblast growth factor receptor 1 (FGFR1), and platelet-derived growth factor receptor β (PDGFR β ) (IC 50 values are 8.4, 39.3 and 98.3 nM respectively). Also inhibits the checkpoint kinases Wee1 and Myt1; abolishes Cdc2 phosphorylation in numerous tumor cell lines and abrogates the G 2 checkpoint.
storage
Desiccate at RT
Properties of PD 166285
Melting point: | 239-242?C |
storage temp. | Desiccate at RT |
solubility | DMSO, Methanol |
form | Pale yellow solid |
color | Yellow |
Stability: | Hygroscopic |
Safety information for PD 166285
Computed Descriptors for PD 166285
New Products
4-AMINO-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID HCL 4-(Dimethylamino)tetrahydro-2H-pyran-4-carbonitrile 4-Aminotetrahydropyran-4-carbonitrile Hydrochloride (R)-3-Aminobutanenitrile Hydrochloride 3-((Dimethylamino)methyl)-5-methylhexan-2-one oxalate 1,4-Dioxa-8-azaspiro[4.5]decane 5-Bromo-2-nitropyridine Nimesulide BP Aceclofenac IP/BP/EP Diclofenac Sodium IP/BP/EP/USP Mefenamic Acid IP/BP/EP/USP Ornidazole IP Diclofenac Potassium THOMAIND PAPER PH 2.0 TO 4.5 1 BOX BUFFER CAPSULE PH 9.2 - 10 CAP SODIUM CHLORIDE 0.1N CVS ALLOXAN MONOHYDRATE 98% PLATINUM 0.5% ON 3 MM ALUMINA PELLETS (TYPE 73) LITHIUM AAS SOLUTION 2-Bromo-1-(bromomethyl)-3-chloro-5-nitrobenzene 2-Bromo-3-nitroaniline N-(3-Hydroxypropyl)-N-methylacetamide 3-Bromo-6-chloropyridazine 4-ethyl-3-nitrobenzoic acidRelated products of tetrahydrofuran
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