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192705-80-9-PD-161570 PD-161570

PD-161570

For research use only. Not for therapeutic Use.

  • CAT Number: I012048
  • CAS Number: 192705-80-9
  • Molecular Formula: C26H35Cl2N7O
  • Molecular Weight: 532.51
  • Purity: ≥95%
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Related Small Molecules: Palmitoyl Tripeptide-1 hydrochloride     human GIP(3-30), amide TFA     Lenvatinib mesylate    

PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively[1][2]. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor[3].
PD-161570 (Compound 6c; 0.1-1 µM; 1-8 days; VSMCs) treatment inhibits PDGF-stimulated vascular smooth muscle cell proliferation in a dose dependent fashion with an IC50 of 0.3 µM on day 8[1].
PD-161570 suppresses constitutive phosphorylation of the FGF-1 receptor in both human ovarian carcinoma cells (A121(p)) and Sf9 insect cells overexpressing the human FGF-1 receptor and blocked the growth of A121(p) cells in culture[2].
PD-161570 can potently inhibit basic fibroblast growth factor (bFGF)-mediated angiogenesis[4].


Catalog Number I012048
CAS Number 192705-80-9
Synonyms

1-tert-butyl-3-[6-(2,6-dichlorophenyl)-2-[4-(diethylamino)butylamino]pyrido[2,3-d]pyrimidin-7-yl]urea

Molecular Formula C26H35Cl2N7O
Purity ≥95%
InChI InChI=1S/C26H35Cl2N7O/c1-6-35(7-2)14-9-8-13-29-24-30-16-17-15-18(21-19(27)11-10-12-20(21)28)23(31-22(17)32-24)33-25(36)34-26(3,4)5/h10-12,15-16H,6-9,13-14H2,1-5H3,(H3,29,30,31,32,33,34,36)
InChIKey MKVMEJKNLUWFSQ-UHFFFAOYSA-N
SMILES CCN(CC)CCCCNC1=NC2=NC(=C(C=C2C=N1)C3=C(C=CC=C3Cl)Cl)NC(=O)NC(C)(C)C
Reference

[1]. Hamby JM, et al. Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors. J Med Chem. 1997 Jul 18;40(15):2296-303.
 [Content Brief]

[2]. Batley BL, et al. Inhibition of FGF-1 receptor tyrosine kinase activity by PD 161570, a new protein-tyrosine kinase inhibitor. Life Sci. 1998;62(2):143-50.
 [Content Brief]

[3]. Kyosuke Hino, et al. An mTOR Signaling Modulator Suppressed Heterotopic Ossification of Fibrodysplasia Ossificans Progressiva. Stem Cell Reports. 2018 Nov 13;11(5):1106-1119.
 [Content Brief]

[4]. Wolfe A, et al. Pharmacologic characterization of a kinetic in vitro human co-culture angiogenesis model using clinically relevant compounds. J Biomol Screen. 2013 Dec;18(10):1234-45.
 [Content Brief]

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