SU4984 | CAS#186610-89-9 | FGFR inhibitor

SU4984
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406474

CAS#: 186610-89-9

Description: SU4984 is a cell-permeable, reversible, and ATP-competitive inhibitor of the tyrosine kinase activity of fibroblast growth factor receptor 1.

Chemical Structure

SU4984

CAS# 186610-89-9

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406474
Name: SU4984
CAS#: 186610-89-9
Chemical Formula: C20H19N3O2
Exact Mass: 333.15
Molecular Weight: 333.380
Elemental Analysis: C, 72.05; H, 5.74; N, 12.60; O, 9.60

Price and Availability

Size	Price	Availability
25mg	USD 250	2 Weeks
50mg	USD 450	2 Weeks
100mg	USD 750	2 Weeks
200mg	USD 1250	2 Weeks
500mg	USD 2650	2 Weeks
1g	USD 3850	2 Weeks
2g	USD 6450	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: SU4984; SU4984; SU 4984.

IUPAC/Chemical Name: (Z)-4-(4-((2-oxoindolin-3-ylidene)methyl)phenyl)piperazine-1-carbaldehyde

InChi Key: ZNFJBJDODKHWED-AQTBWJFISA-N

InChi Code: InChI=1S/C20H19N3O2/c24-14-22-9-11-23(12-10-22)16-7-5-15(6-8-16)13-18-17-3-1-2-4-19(17)21-20(18)25/h1-8,13-14H,9-12H2,(H,21,25)/b18-13-

SMILES Code: O=CN1CCN(C2=CC=C(/C=C3C(NC4=C\3C=CC=C4)=O)C=C2)CC1

Appearance: Yellow 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, not in water

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:	SU4984 has an IC50 of 10-20 μM for fibroblast growth factor receptor 1 (FGFR1).
In vitro activity:	SU4984, SU6577, and SU5614 were effective against KIT with juxtamembrane activating mutations, but only SU6577 could suppress KIT containing either juxtamembrane or kinase domain activating mutations. SU4984, SU6577, and SU5614 killed neoplastic mast cells expressing a juxtamembrane-mutated KIT. SU4984 and SU6577 killed neoplastic mast cells expressing KIT bearing a kinase domain mutation. Reference: J Invest Dermatol. 2000 Feb;114(2):392-4. https://pubmed.ncbi.nlm.nih.gov/10652004/
In vivo activity:	To be determined

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	50.0	149.98

Preparing Stock Solutions

The following data is based on the product molecular weight 333.38 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.

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. Chen G, Weng Q, Fu L, Wang Z, Yu P, Liu Z, Li X, Zhang H, Liang G. Synthesis and biological evaluation of novel oxindole-based RTK inhibitors as anti-cancer agents. Bioorg Med Chem. 2014 Dec 15;22(24):6953-60. doi: 10.1016/j.bmc.2014.10.017. Epub 2014 Oct 29. PMID: 25456085. 2. Ma Y, Carter E, Wang X, Shu C, McMahon G, Longley BJ. Indolinone derivatives inhibit constitutively activated KIT mutants and kill neoplastic mast cells. J Invest Dermatol. 2000 Feb;114(2):392-4. doi: 10.1046/j.1523-1747.2000.00888.x. PMID: 10652004.
In vitro protocol:	1. Chen G, Weng Q, Fu L, Wang Z, Yu P, Liu Z, Li X, Zhang H, Liang G. Synthesis and biological evaluation of novel oxindole-based RTK inhibitors as anti-cancer agents. Bioorg Med Chem. 2014 Dec 15;22(24):6953-60. doi: 10.1016/j.bmc.2014.10.017. Epub 2014 Oct 29. PMID: 25456085. 2. Ma Y, Carter E, Wang X, Shu C, McMahon G, Longley BJ. Indolinone derivatives inhibit constitutively activated KIT mutants and kill neoplastic mast cells. J Invest Dermatol. 2000 Feb;114(2):392-4. doi: 10.1046/j.1523-1747.2000.00888.x. PMID: 10652004.
In vivo protocol:	To be determined

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

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1: Matsuo M, Yamada S, Koizumi K, Sakurai H, Saiki I. Tumour-derived fibroblast growth factor-2 exerts lymphangiogenic effects through Akt/mTOR/p70S6kinase pathway in rat lymphatic endothelial cells. Eur J Cancer. 2007 Jul;43(11):1748-54. Epub 2007 Jun 13. PubMed PMID: 17570654.

2: Mologni L, Sala E, Cazzaniga S, Rostagno R, Kuoni T, Puttini M, Bain J, Cleris L, Redaelli S, Riva B, Formelli F, Scapozza L, Gambacorti-Passerini C. Inhibition of RET tyrosine kinase by SU5416. J Mol Endocrinol. 2006 Oct;37(2):199-212. PubMed PMID: 17032739.

3: Welsh M, Welsh C, Ekman M, Dixelius J, HÃ¤gerkvist R, AnnerÃ©n C, Akerblom B, Mahboobi S, Chandrasekharan S, Liu ET. The tyrosine kinase FRK/RAK participates in cytokine-induced islet cell cytotoxicity. Biochem J. 2004 Aug 15;382(Pt 1):261-8. PubMed PMID: 15186217; PubMed Central PMCID: PMC1133939.

4: Fuhrmann G, Leisser C, Rosenberger G, Grusch M, Huettenbrenner S, Halama T, Mosberger I, Sasgary S, Cerni C, Krupitza G. Cdc25A phosphatase suppresses apoptosis induced by serum deprivation. Oncogene. 2001 Jul 27;20(33):4542-53. PubMed PMID: 11494150.

5: Longley BJ, Ma Y, Carter E, McMahon G. New approaches to therapy for mastocytosis. A case for treatment with kit kinase inhibitors. Hematol Oncol Clin North Am. 2000 Jun;14(3):689-95. Review. PubMed PMID: 10909046.

6: Ma Y, Carter E, Wang X, Shu C, McMahon G, Longley BJ. Indolinone derivatives inhibit constitutively activated KIT mutants and kill neoplastic mast cells. J Invest Dermatol. 2000 Feb;114(2):392-4. PubMed PMID: 10652004.

7: Toledo LM, Lydon NB, Elbaum D. The structure-based design of ATP-site directed protein kinase inhibitors. Curr Med Chem. 1999 Sep;6(9):775-805. Review. PubMed PMID: 10495352.

8: D'Jamoos CA, McMahon G, Tsonis PA. Fibroblast growth factor receptors regulate the ability for hindlimb regeneration in Xenopus laevis. Wound Repair Regen. 1998 Jul-Aug;6(4):388-97. PubMed PMID: 9824558.

9: Mohammadi M, McMahon G, Sun L, Tang C, Hirth P, Yeh BK, Hubbard SR, Schlessinger J. Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors. Science. 1997 May 9;276(5314):955-60. PubMed PMID: 9139660.

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