PD-161570
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MedKoo CAT#: 407384

CAS#: 192705-80-9

Description: PD-161570 is a selective FGFR inhibitor (IC50 values are 40, 262 and 3700 nM for FGFR, PDGFR and EGFR respectively). PD 161570 had about 5- and 100-fold greater selectivity toward the FGF-1 receptor (IC50 = 40 nM) compared with the PDGFbeta receptor (IC50 = 262 nM) or EGF receptor (IC50 = 3.7 microM) tyrosine kinases, respectively. In addition, PD 161570 suppressed 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. The results demonstrate a novel synthetic inhibitor with nanomolar potency and specificity towards the FGF-1 receptor tyrosine kinase.

Chemical Structure

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PD-161570
CAS# 192705-80-9
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 407384
Name: PD-161570
CAS#: 192705-80-9
Chemical Formula: C26H35Cl2N7O
Exact Mass: 531.23
Molecular Weight: 532.514
Elemental Analysis: C, 58.64; H, 6.63; Cl, 13.31; N, 18.41; O, 3.00

Price and Availability

Size Price Availability Quantity
5mg USD 285 2 Weeks
10mg USD 500 2 Weeks
25mg USD 800 2 Weeks
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Synonym: PD-161570; PD 161570; PD161570.

IUPAC/Chemical Name: N-[6-(2,6-Dichlorophenyl)-2-[[4-(diethylamino)butyl]amino]pyrido[2,3-d]pyrimidin-7-yl]-N'-(1,1-dimethylethyl)urea

InChi Key: MKVMEJKNLUWFSQ-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: O=C(NC(C)(C)C)NC1=NC2=NC(NCCCCN(CC)CC)=NC=C2C=C1C3=C(Cl)C=CC=C3Cl

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Product Data
Certificate of Analysis:
View CoA: current batch, Lot#C9M04C16
Safety Data Sheet (SDS):
View Safety Data Sheet (SDS)
Instruction:
View handling instruction
Biological target: 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.
In vitro activity: 1-Tert-butyl-3-[6-(2,6-dichloro-phenyl)-2-(4-diethylamino-butylamino)-py rido[2,3-d]pyrimidin-7-yl]-urea (PD 161570) had about 5- and 100-fold greater selectivity toward the FGF-1 receptor (IC50 = 40 nM) compared with the PDGFbeta receptor (IC50 = 262 nM) or EGF receptor (IC50 = 3.7 microM) tyrosine kinases, respectively. In addition, PD 161570 suppressed 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. Reference: Life Sci. 1998;62(2):143-50. https://pubmed.ncbi.nlm.nih.gov/9488112/
In vivo activity: TBD

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 43.3 81.29
Ethanol 53.3 100.00

Preparing Stock Solutions

The following data is based on the product molecular weight 532.51 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Wolfe A, O'Clair B, Groppi VE, McEwen DP. 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. doi: 10.1177/1087057113502085. Epub 2013 Sep 9. PMID: 24019254. 2. Batley BL, Doherty AM, Hamby JM, Lu GH, Keller P, Dahring TK, Hwang O, Crickard K, Panek RL. Inhibition of FGF-1 receptor tyrosine kinase activity by PD 161570, a new protein-tyrosine kinase inhibitor. Life Sci. 1998;62(2):143-50. doi: 10.1016/s0024-3205(97)01060-6. PMID: 9488112.
In vitro protocol: 1. Wolfe A, O'Clair B, Groppi VE, McEwen DP. 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. doi: 10.1177/1087057113502085. Epub 2013 Sep 9. PMID: 24019254. 2. Batley BL, Doherty AM, Hamby JM, Lu GH, Keller P, Dahring TK, Hwang O, Crickard K, Panek RL. Inhibition of FGF-1 receptor tyrosine kinase activity by PD 161570, a new protein-tyrosine kinase inhibitor. Life Sci. 1998;62(2):143-50. doi: 10.1016/s0024-3205(97)01060-6. PMID: 9488112.
In vivo protocol: TBD

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1: Batley BL, Doherty AM, Hamby JM, Lu GH, Keller P, Dahring TK, Hwang O,
Crickard K, Panek RL. Inhibition of FGF-1 receptor tyrosine kinase activity by PD
161570, a new protein-tyrosine kinase inhibitor. Life Sci. 1998;62(2):143-50.
PubMed PMID: 9488112.


2: Saksena S, Priyamvada S, Kumar A, Akhtar M, Soni V, Anbazhagan AN, Alakkam A,
Alrefai WA, Dudeja PK, Gill RK. Keratinocyte growth factor-2 stimulates
P-glycoprotein expression and function in intestinal epithelial cells. Am J
Physiol Gastrointest Liver Physiol. 2013 Mar 15;304(6):G615-22. doi:
10.1152/ajpgi.00445.2012. PubMed PMID: 23328208; PubMed Central PMCID:
PMC3602685.


3: Wolfe A, O'Clair B, Groppi VE, McEwen DP. 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. doi:
10.1177/1087057113502085. PubMed PMID: 24019254.


4: Stevens DA, Harvey CB, Scott AJ, O'Shea PJ, Barnard JC, Williams AJ, Brady G,
Samarut J, Chassande O, Williams GR. Thyroid hormone activates fibroblast growth
factor receptor-1 in bone. Mol Endocrinol. 2003 Sep;17(9):1751-66. PubMed PMID:
12805413.


5: Hamby JM, Connolly CJ, Schroeder MC, Winters RT, Showalter HD, Panek RL, Major
TC, Olsewski B, Ryan MJ, Dahring T, Lu GH, Keiser J, Amar A, Shen C, Kraker AJ,
Slintak V, Nelson JM, Fry DW, Bradford L, Hallak H, Doherty AM.
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. PubMed PMID:
9240345.