SU11274 | CAS#658084-23-2 | MET inhibitor

MedKoo Cat#: 402150 | Name: SU11274

Featured

Description:

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

SU11274 is a selective Met tyrosine kinase inhibitor with IC50 of 10 nM. SU11274 increases tumorigenicity and enriched for melanoma-initiating cells by bioenergetic modulation. SU11274 suppresses proliferation and motility of pancreatic cancer cells. SU11274 enhances the response of the prostate cancer cell line DU145 to ionizing radiation. SU11274 exhibits a selective inhibition pattern toward different receptor mutated variants.

Chemical Structure

SU11274

CAS#658084-23-2

Theoretical Analysis

MedKoo Cat#: 402150

Name: SU11274

CAS#: 658084-23-2

Chemical Formula: C28H30ClN5O4S

Exact Mass: 567.1707

Molecular Weight: 568.09

Elemental Analysis: C, 59.20; H, 5.32; Cl, 6.24; N, 12.33; O, 11.27; S, 5.64

Price and Availability

Size	Price	Availability
25mg	USD 450.00	2 Weeks
50mg	USD 750.00	2 Weeks
100mg	USD 1,250.00	2 Weeks

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

No Data

Synonym

SU 11274; SU11274; SU-11274.

IUPAC/Chemical Name

(3Z)-N-(3-Chlorophenyl)-3-[[3,5-dimethyl-4-[(4-methyl-1-piperazinyl)carbonyl]-1H-pyrrol-2-yl]methylene]-2,3-dihydro-N-methyl-2-oxo-1H-indole-5-sulfonamide

InChi Key

FPYJSJDOHRDAMT-KQWNVCNZSA-N

InChi Code

InChI=1S/C28H30ClN5O4S/c1-17-25(30-18(2)26(17)28(36)34-12-10-32(3)11-13-34)16-23-22-15-21(8-9-24(22)31-27(23)35)39(37,38)33(4)20-7-5-6-19(29)14-20/h5-9,14-16,30H,10-13H2,1-4H3,(H,31,35)/b23-16-

SMILES Code

O=S(C1=CC2=C(NC(/C2=C\C3=C(C)C(C(N4CCN(C)CC4)=O)=C(C)N3)=O)C=C1)(N(C5=CC=CC(Cl)=C5)C)=O

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, not in water

Shelf Life

>5 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:

SU11274 is an inhibitor of c-Met (IC50 = 20 nM) with little or no activity against other receptor tyrosine kinases. SU11274 induces apoptosis and cell cycle arrest in transformed Ba/F3 cells and cancer cell lines.

In vitro activity:

SU11274 suppresses the proliferation of pancreatic cancer cells via the downregulation of cyclin D1. Following SU11274 treatment, the proliferation of MIA-Paca2 and PK-45H cells was suppressed to 19.8±10.7% and 45.8±14.8%, respectively. Cyclin D1 expression was downregulated to 43.7±17.9% and 53.2±18.6% in the MIA-Paca2 and PK-45H cell lines, respectively, following SU11274 treatment. Cell motility was reduced to 1.0±0.3% in MIA-Paca2 and 14.7±3.5% in PK-45H following SU11274 treatment. Reference: Oncol Lett. 2015 Sep;10(3):1468-1472. https://pubmed.ncbi.nlm.nih.gov/26622692/

In vivo activity:

SU11274 increased tumorigenicity and enriched for melanoma-initiating cells by bioenergetic modulation. In an xenograft model, SU11274 substantially decreased number of cells in adherent and spheroid cultures, but increased their tumorigenic potential as determined by higher frequency of tumor-initiating cells. SU11274 treatment was not associated with any significant alteration in the expression of stem cell markers, but it stimulated higher level of pluripotent markers. Reference: BMC Cancer. 2016 May 12;16:308. https://pubmed.ncbi.nlm.nih.gov/27175734/

	Solvent	mg/mL	mM
Solubility
	DMF	20.0	35.21
	DMF:PBS (pH 7.2) (1:4)	0.2	0.35
	DMSO	11.0	19.36
	Ethanol	0.3	0.44

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 568.09 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. Tomizawa M, Shinozaki F, Motoyoshi Y, Sugiyama T, Yamamoto S, Ishige N. SU11274 suppresses proliferation and motility of pancreatic cancer cells. Oncol Lett. 2015 Sep;10(3):1468-1472. doi: 10.3892/ol.2015.3452. Epub 2015 Jul 2. PMID: 26622692; PMCID: PMC4533741. 2. Yu H, Li X, Sun S, Gao X, Zhou D. c-Met inhibitor SU11274 enhances the response of the prostate cancer cell line DU145 to ionizing radiation. Biochem Biophys Res Commun. 2012 Oct 26;427(3):659-65. doi: 10.1016/j.bbrc.2012.09.117. Epub 2012 Sep 28. PMID: 23026049. 3. Kucerova L, Demkova L, Skolekova S, Bohovic R, Matuskova M. Tyrosine kinase inhibitor SU11274 increased tumorigenicity and enriched for melanoma-initiating cells by bioenergetic modulation. BMC Cancer. 2016 May 12;16:308. doi: 10.1186/s12885-016-2341-y. PMID: 27175734; PMCID: PMC4866285. 4. Kenessey I, Keszthelyi M, Krámer Z, Berta J, Adám A, Dobos J, Mildner M, Flachner B, Cseh S, Barna G, Szokol B, Orfi L, Kéri G, Döme B, Klepetko W, Tímár J, Tóvári J. Inhibition of c-Met with the specific small molecule tyrosine kinase inhibitor SU11274 decreases growth and metastasis formation of experimental human melanoma. Curr Cancer Drug Targets. 2010 May;10(3):332-42. doi: 10.2174/156800910791190184. PMID: 20370683.

In vitro protocol:

In vivo protocol:

1. Kucerova L, Demkova L, Skolekova S, Bohovic R, Matuskova M. Tyrosine kinase inhibitor SU11274 increased tumorigenicity and enriched for melanoma-initiating cells by bioenergetic modulation. BMC Cancer. 2016 May 12;16:308. doi: 10.1186/s12885-016-2341-y. PMID: 27175734; PMCID: PMC4866285. 2. Kenessey I, Keszthelyi M, Krámer Z, Berta J, Adám A, Dobos J, Mildner M, Flachner B, Cseh S, Barna G, Szokol B, Orfi L, Kéri G, Döme B, Klepetko W, Tímár J, Tóvári J. Inhibition of c-Met with the specific small molecule tyrosine kinase inhibitor SU11274 decreases growth and metastasis formation of experimental human melanoma. Curr Cancer Drug Targets. 2010 May;10(3):332-42. doi: 10.2174/156800910791190184. PMID: 20370683.

1: Zhang Y, Li X, Yu Q, Lv X, Li C, Wang L, Liu Y, Wang Q, Yang Z, Fu X, Xiao R. Using network pharmacology to discover potential drugs for hypertrophic scars. Br J Dermatol. 2024 Sep 18;191(4):592-604. doi: 10.1093/bjd/ljae234. PMID: 38820210. 2: Zhou SR, Zhu YS, Yuan WT, Pan XY, Wang T, Chen XD. Hepatocyte growth factor promotes retinal pigment epithelium cell activity through MET/AKT signaling pathway. Int J Ophthalmol. 2024 May 18;17(5):806-814. doi: 10.18240/ijo.2024.05.03. PMID: 38766346; PMCID: PMC11074208. 3: Wang Q, Li Y, Yuan H, Peng L, Dai Z, Sun Y, Liu R, Li W, Li J, Zhu C. Hypoxia preconditioning of human amniotic mesenchymal stem cells enhances proliferation and migration and promotes their homing via the HGF/C-MET signaling axis to augment the repair of acute liver failure. Tissue Cell. 2024 Apr;87:102326. doi: 10.1016/j.tice.2024.102326. Epub 2024 Feb 17. PMID: 38442547. 4: Lee YY, Ryu JY, Cho YJ, Choi JY, Choi JJ, Choi CH, Sa JK, Hwang JR, Lee JW. The anti-tumor effects of AZD4547 on ovarian cancer cells: differential responses based on c-Met and FGF19/FGFR4 expression. Cancer Cell Int. 2024 Jan 25;24(1):43. doi: 10.1186/s12935-024-03235-2. PMID: 38273381; PMCID: PMC10811874. 5: Lang L, Chen F, Li Y, Shay C, Yang F, Dan H, Chen ZG, Saba NF, Teng Y. Adaptive c-Met-PLXDC2 Signaling Axis Mediates Cancer Stem Cell Plasticity to Confer Radioresistance-associated Aggressiveness in Head and Neck Cancer. Cancer Res Commun. 2023 Apr 19;3(4):659-671. doi: 10.1158/2767-9764.CRC-22-0289. PMID: 37089864; PMCID: PMC10114932. 6: Novoa Díaz MB, Carriere P, Gigola G, Zwenger AO, Calvo N, Gentili C. Involvement of Met receptor pathway in aggressive behavior of colorectal cancer cells induced by parathyroid hormone-related peptide. World J Gastroenterol. 2022 Jul 14;28(26):3177-3200. doi: 10.3748/wjg.v28.i26.3177. PMID: 36051345; PMCID: PMC9331538. 7: Tao X, Chen C, Chen Y, Zhang L, Hu J, Yu H, Liang M, Fu Q, Huang K. β2-adrenergic receptor promotes liver regeneration partially through crosstalk with c-met. Cell Death Dis. 2022 Jun 27;13(6):571. doi: 10.1038/s41419-022-04998-0. PMID: 35760785; PMCID: PMC9237079. 8: Chen X, Tian F, Lun P, Feng Y. Curcumin Inhibits HGF-Induced EMT by Regulating c-MET-Dependent PI3K/Akt/mTOR Signaling Pathways in Meningioma. Evid Based Complement Alternat Med. 2021 Aug 6;2021:5574555. doi: 10.1155/2021/5574555. PMID: 34408780; PMCID: PMC8367536. 9: Nelhűbel GA, Cserepes M, Szabó B, Türk D, Kárpáti A, Kenessey I, Rásó E, Barbai T, Hegedűs Z, László V, Szokol B, Dobos J, Őrfi L, Tóvári J. EGFR Alterations Influence the Cetuximab Treatment Response and c-MET Tyrosine-Kinase Inhibitor Sensitivity in Experimental Head and Neck Squamous Cell Carcinomas. Pathol Oncol Res. 2021 May 3;27:620256. doi: 10.3389/pore.2021.620256. PMID: 34257586; PMCID: PMC8262169. 10: Cserepes M, Nelhűbel GA, Meilinger-Dobra M, Surguta SE, Rásó E, Ladányi A, Kenessey I, Szöőr Á, Vereb G, Remenár É, Tóvári J. Az EGFR extracelluláris módosulásainak hatása fej-nyaki daganatok cetuximabterápiájára [Consequences of extracellular alterations of EGFR on cetuximab therapy in HNSCC]. Magy Onkol. 2021 Jun 3;65(2):188-195. Hungarian. Epub 2021 May 12. PMID: 34081766. 11: Huang C, Zheng Y, Bai J, Shi C, Shi X, Shan H, Zhou X. Hepatocyte growth factor overexpression promotes osteoclastogenesis and exacerbates bone loss in CIA mice. J Orthop Translat. 2020 Dec 10;27:9-16. doi: 10.1016/j.jot.2020.10.011. PMID: 33344167; PMCID: PMC7732867. 12: Chen S, Wang Y, Chen L, Xia Y, Cui J, Wang W, Jiang X, Wang J, Zhu Y, Sun S, Zou Y, Gong Y, Shi B. CUL4B promotes aggressive phenotypes of renal cell carcinoma via upregulating c-Met expression. Int J Biochem Cell Biol. 2021 Jan;130:105887. doi: 10.1016/j.biocel.2020.105887. Epub 2020 Nov 20. PMID: 33227394. 13: Miao YM, Zhang YJ, Qiao SM, Xia YF, Wei ZF, Dai Y. Oral administration of curcumin ameliorates pulmonary fibrosis in mice through 15d-PGJ2-mediated induction of hepatocyte growth factor in the colon. Acta Pharmacol Sin. 2021 Mar;42(3):422-435. doi: 10.1038/s41401-020-0469-4. Epub 2020 Jul 21. PMID: 32694760; PMCID: PMC8027789. 14: Koustas E, Karamouzis MV, Sarantis P, Schizas D, Papavassiliou AG. Inhibition of c-MET increases the antitumour activity of PARP inhibitors in gastric cancer models. J Cell Mol Med. 2020 Sep;24(18):10420-10431. doi: 10.1111/jcmm.15655. Epub 2020 Jul 20. PMID: 32686903; PMCID: PMC7521333. 15: Tang H, Gamdzyk M, Huang L, Gao L, Lenahan C, Kang R, Tang J, Xia Y, Zhang JH. Delayed recanalization after MCAO ameliorates ischemic stroke by inhibiting apoptosis via HGF/c-Met/STAT3/Bcl-2 pathway in rats. Exp Neurol. 2020 Aug;330:113359. doi: 10.1016/j.expneurol.2020.113359. Epub 2020 May 16. PMID: 32428505. 16: Hamza GM, Bergo VB, Mamaev S, Wojchowski DM, Toran P, Worsfold CR, Castaldi MP, Silva JC. Affinity-Bead Assisted Mass Spectrometry (Affi-BAMS): A Multiplexed Microarray Platform for Targeted Proteomics. Int J Mol Sci. 2020 Mar 16;21(6):2016. doi: 10.3390/ijms21062016. PMID: 32188029; PMCID: PMC7139916. 17: Li Y, Zhou H, Chen Y, Zhong D, Su P, Yuan H, Yang X, Liao Z, Qiu X, Wang X, Liang T, Gao W, Shen X, Zhang X, Lian C, Xu C. MET promotes the proliferation and differentiation of myoblasts. Exp Cell Res. 2020 Mar 15;388(2):111838. doi: 10.1016/j.yexcr.2020.111838. Epub 2020 Jan 10. PMID: 31930964. 18: Tong X, Liang R, Jia Y, Qin W, Guo C, Wu X, Wang Z, Chen D, Tan N. Suhuang Antitussive Capsules-Ameliorative Effects on LPS-Induced Sputum Obstruction in Mice Through Promoting HGF Secretion. Front Pharmacol. 2019 Dec 19;10:1422. doi: 10.3389/fphar.2019.01422. PMID: 31920638; PMCID: PMC6930918. 19: Tong G, Cheng B, Li J, Wu X, Nong Q, He L, Li X, Li L, Wang S. MACC1 regulates PDL1 expression and tumor immunity through the c-Met/AKT/mTOR pathway in gastric cancer cells. Cancer Med. 2019 Nov;8(16):7044-7054. doi: 10.1002/cam4.2542. Epub 2019 Sep 26. PMID: 31557409; PMCID: PMC6853821. 20: Serova OV, Orsa AN, Chachina NA, Petrenko AG, Deyev IE. с-Met receptor can be activated by extracellular alkaline medium. J Recept Signal Transduct Res. 2019 Feb;39(1):67-72. doi: 10.1080/10799893.2019.1620775. Epub 2019 Jun 19. PMID: 31215287.