MedKoo Cat#: 202710 | Name: SU14813
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Description:

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

SU14813 is an oral, multitargeted tyrosine kinase inhibitor (TKI) targeting vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR), KIT, and fms-like tyrosine kinase 3 (FLT-3) (1). SU14813 was developed as a next-generation TKI agent following sunitinib (SU11248) designed to demonstrate optimized pharmacokinetic (PK) and tolerability profiles. SU14813 demonstrated broad and potent antitumor activity equivalent to that of sunitinib, which resulted in tumor regression, growth arrest, growth delay, and prolonged survival in established xenograft cancer models in mice.

Chemical Structure

SU14813
SU14813
CAS#627908-92-3 (free base)

Theoretical Analysis

MedKoo Cat#: 202710

Name: SU14813

CAS#: 627908-92-3 (free base)

Chemical Formula: C23H27FN4O4

Exact Mass: 442.2016

Molecular Weight: 442.48

Elemental Analysis: C, 62.43; H, 6.15; F, 4.29; N, 12.66; O, 14.46

Price and Availability

Size Price Availability Quantity
10mg USD 150.00 Ready to ship
25mg USD 250.00 Ready to ship
50mg USD 450.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,250.00 Ready to ship
500mg USD 2,650.00 Ready to ship
1g USD 4,250.00 Ready to ship
2g USD 6,750.00 Ready to ship
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Related CAS #
452105-23-6 (Z isomer) 627908-92-3 (free base) 849643-15-8 (maleate)
Synonym
SU14813; SU 14813; SU-14813; SU014813; SU-014813; SU 014813
IUPAC/Chemical Name
(S,Z)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-N-(2-hydroxy-3-morpholinopropyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide
InChi Key
CTNPALGJUAXMMC-PMFHANACSA-N
InChi Code
InChI=1S/C23H27FN4O4/c1-13-20(10-18-17-9-15(24)3-4-19(17)27-22(18)30)26-14(2)21(13)23(31)25-11-16(29)12-28-5-7-32-8-6-28/h3-4,9-10,16,26,29H,5-8,11-12H2,1-2H3,(H,25,31)(H,27,30)/b18-10-/t16-/m0/s1
SMILES Code
O=C(C1=C(C)NC(/C=C2C(NC3=C\2C=C(F)C=C3)=O)=C1C)NC[C@H](O)CN4CCOCC4
Appearance
white 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
Related CAS# 452105-23-6 ( SU14813 double Z isomer) 627908-92-3 (SU1481free base); 849643-15-8 (SU1481 maleate)                                     
Biological target:
SU14813 is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
In vitro activity:
SU14813 inhibited cellular ligand-dependent phosphorylation of VEGFR-2 (transfected NIH 3T3 cells), PDGFR-β (transfected NIH 3T3 cells), KIT (Mo7e cells), and FLT3-internal tandem duplication (FLT3-ITD; MV4;11 cells) as well as FMS/CSF1R (transfected NIH 3T3 cells), another split-kinase RTK. SU14813 inhibited VEGFR-2, PDGFR-β, and KIT phosphorylation in porcine aorta endothelial cells overexpressing these targets, with cellular IC50 values of 5.2, 9.9, and 11.2 nmol/L, respectively. Reference: Mol Cancer Ther. 2006 Jul;5(7):1774-82. https://pubmed.ncbi.nlm.nih.gov/16891463/
In vivo activity:
In xenograft models, SU14813 exhibited dose-dependent antitumor efficacy, resulting in regression of 786-O (PDGFR, VEGFR-expressing) and MV4;11 (activated FLT3-dependent) tumors, growth arrest of Colo205 tumors, and growth delay of C6 (PDGFR-expressing) and MV522 tumors). In a murine leukemia model, SU14813 treatment conferred an approximate doubling of survival time from 23 to 42 days at these dose levels. Reference: Mol Cancer Ther. 2006 Jul;5(7):1774-82. https://pubmed.ncbi.nlm.nih.gov/16891463/
Solvent mg/mL mM
Solubility
DMSO 54.0 122.04
DMF 30.0 67.80
Ethanol 0.1 0.23
PBS (pH 7.2) 0.1 0.23
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 442.48 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. Lee E, Rewolinski D. Evaluation of CXCR4 inhibition in the prevention and intervention model of laser-induced choroidal neovascularization. Invest Ophthalmol Vis Sci. 2010 Jul;51(7):3666-72. doi: 10.1167/iovs.09-3802. Epub 2009 Dec 30. PMID: 20042641. 2. Patyna S, Laird AD, Mendel DB, O'farrell AM, Liang C, Guan H, Vojkovsky T, Vasile S, Wang X, Chen J, Grazzini M, Yang CY, Haznedar JO, Sukbuntherng J, Zhong WZ, Cherrington JM, Hu-Lowe D. SU14813: a novel multiple receptor tyrosine kinase inhibitor with potent antiangiogenic and antitumor activity. Mol Cancer Ther. 2006 Jul;5(7):1774-82. doi: 10.1158/1535-7163.MCT-05-0333. PMID: 16891463. 3. Fiedler W, Giaccone G, Lasch P, van der Horst I, Brega N, Courtney R, Abbattista A, Shalinsky DR, Bokemeyer C, Boven E. Phase I trial of SU14813 in patients with advanced solid malignancies. Ann Oncol. 2011 Jan;22(1):195-201. doi: 10.1093/annonc/mdq313. Epub 2010 Jul 6. PMID: 20605934.
In vitro protocol:
1. Lee E, Rewolinski D. Evaluation of CXCR4 inhibition in the prevention and intervention model of laser-induced choroidal neovascularization. Invest Ophthalmol Vis Sci. 2010 Jul;51(7):3666-72. doi: 10.1167/iovs.09-3802. Epub 2009 Dec 30. PMID: 20042641. 2. Patyna S, Laird AD, Mendel DB, O'farrell AM, Liang C, Guan H, Vojkovsky T, Vasile S, Wang X, Chen J, Grazzini M, Yang CY, Haznedar JO, Sukbuntherng J, Zhong WZ, Cherrington JM, Hu-Lowe D. SU14813: a novel multiple receptor tyrosine kinase inhibitor with potent antiangiogenic and antitumor activity. Mol Cancer Ther. 2006 Jul;5(7):1774-82. doi: 10.1158/1535-7163.MCT-05-0333. PMID: 16891463.
In vivo protocol:
1. Fiedler W, Giaccone G, Lasch P, van der Horst I, Brega N, Courtney R, Abbattista A, Shalinsky DR, Bokemeyer C, Boven E. Phase I trial of SU14813 in patients with advanced solid malignancies. Ann Oncol. 2011 Jan;22(1):195-201. doi: 10.1093/annonc/mdq313. Epub 2010 Jul 6. PMID: 20605934. 2. Patyna S, Laird AD, Mendel DB, O'farrell AM, Liang C, Guan H, Vojkovsky T, Vasile S, Wang X, Chen J, Grazzini M, Yang CY, Haznedar JO, Sukbuntherng J, Zhong WZ, Cherrington JM, Hu-Lowe D. SU14813: a novel multiple receptor tyrosine kinase inhibitor with potent antiangiogenic and antitumor activity. Mol Cancer Ther. 2006 Jul;5(7):1774-82. doi: 10.1158/1535-7163.MCT-05-0333. PMID: 16891463.