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MedKoo Cat#: 341194 | Name: NP603
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

NP603 is a cell-permeable inhibitor of PDGFRβ, FGFR1 and VEGFR2 that binds to ATP pocket. NP603 is a very weak inhibitor of EGFR

Chemical Structure

NP603
NP603
CAS#949164-80-1

Theoretical Analysis

MedKoo Cat#: 341194

Name: NP603

CAS#: 949164-80-1

Chemical Formula: C26H26N2O5

Exact Mass: 446.1842

Molecular Weight: 446.50

Elemental Analysis: C, 69.94; H, 5.87; N, 6.27; O, 17.92

Price and Availability

Size Price Availability Quantity
5mg USD 325.00
25mg USD 890.00
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Related CAS #
No Data
Synonym
NP603; NP-603; NP 603.
IUPAC/Chemical Name
(Z)-3-(5-(6-(3,5-Dimethoxyphenyl)-2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-2,4-dimethyl-1H-pyrrol-3-yl)-propionic acid, 5-[[6-(3,5-Dimethoxyphenyl)-1,2-dihydro-2-oxo-3H-indol-3-ylidene]methyl]-2,4-dimethyl-1H-pyrrole-3-propanoic acid
InChi Key
ZIZSHSPAAJIYOD-XKZIYDEJSA-N
InChi Code
InChI=1S/C26H26N2O5/c1-14-20(7-8-25(29)30)15(2)27-23(14)13-22-21-6-5-16(11-24(21)28-26(22)31)17-9-18(32-3)12-19(10-17)33-4/h5-6,9-13,27H,7-8H2,1-4H3,(H,28,31)(H,29,30)/b22-13-
SMILES Code
CC(C(CCC(O)=O)=C(N1)C)=C1/C=C(C(O)=N2)/C3=C2C=C(C4=CC(OC)=CC(OC)=C4)C=C3
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
Instruction
View handling instruction
Biological target:
NP603 is a cell-permeable inhibitor of PDGFRβ, FGFR1 and VEGFR2 that binds to ATP pocket.
In vitro activity:
NP603 was synthesized and found to be more active against endothelial proliferation of HUVEC after the rhFGF-2 stimulation than SU6668 with minimum effective dose of 0.4 microM but with similar potency as SU16g. NP603 inhibited the tyrosine phosphorylation in FGF receptor and the activation of extracellular signal-regulated kinase and c-Jun-N-terminal-kinase after the rhFGF-2 stimulation. Reference: Bioorg Med Chem Lett. 2007 Sep 1;17(17):4812-8. https://pubmed.ncbi.nlm.nih.gov/17618113/
In vivo activity:
Given the above findings, this study next asked whether NP603 could reverse liver fibrogenesis in vivo following CCl4 administration. Liver tissue morphometry after trichrome staining demonstrated that NP603 (40 mg·kg−1·day−1) treatment significantly decreased hepatic ECM deposition (Fig. 7, C and D). NP603 treatment reduced α-SMA immunoreactivity and mRNA expression by 67% and 70%, respectively (Fig. 8, B and C). Reference: Am J Physiol Cell Physiol. 2011 Aug;301(2):C469-77. https://pubmed.ncbi.nlm.nih.gov/21543745/

Preparing Stock Solutions

The following data is based on the product molecular weight 446.50 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. Kammasud N, Boonyarat C, Tsunoda S, Sakurai H, Saiki I, Grierson DS, Vajragupta O. Novel inhibitor for fibroblast growth factor receptor tyrosine kinase. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4812-8. doi: 10.1016/j.bmcl.2007.06.058. Epub 2007 Jun 26. PMID: 17618113. 2. Lin N, Chen S, Pan W, Xu L, Hu K, Xu R. NP603, a novel and potent inhibitor of FGFR1 tyrosine kinase, inhibits hepatic stellate cell proliferation and ameliorates hepatic fibrosis in rats. Am J Physiol Cell Physiol. 2011 Aug;301(2):C469-77. doi: 10.1152/ajpcell.00452.2010. Epub 2011 May 4. PMID: 21543745.
In vitro protocol:
Kammasud N, Boonyarat C, Tsunoda S, Sakurai H, Saiki I, Grierson DS, Vajragupta O. Novel inhibitor for fibroblast growth factor receptor tyrosine kinase. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4812-8. doi: 10.1016/j.bmcl.2007.06.058. Epub 2007 Jun 26. PMID: 17618113.
In vivo protocol:
Lin N, Chen S, Pan W, Xu L, Hu K, Xu R. NP603, a novel and potent inhibitor of FGFR1 tyrosine kinase, inhibits hepatic stellate cell proliferation and ameliorates hepatic fibrosis in rats. Am J Physiol Cell Physiol. 2011 Aug;301(2):C469-77. doi: 10.1152/ajpcell.00452.2010. Epub 2011 May 4. PMID: 21543745.
1: Lin N, Chen S, Pan W, Xu L, Hu K, Xu R. NP603, a novel and potent inhibitor of FGFR1 tyrosine kinase, inhibits hepatic stellate cell proliferation and ameliorates hepatic fibrosis in rats. Am J Physiol Cell Physiol. 2011 Aug;301(2):C469-77. doi: 10.1152/ajpcell.00452.2010. Epub 2011 May 4. PubMed PMID: 21543745. 2: Kammasud N, Boonyarat C, Tsunoda S, Sakurai H, Saiki I, Grierson DS, Vajragupta O. Novel inhibitor for fibroblast growth factor receptor tyrosine kinase. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4812-8. Epub 2007 Jun 26. PubMed PMID: 17618113.

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