SU11274 (SU-11274)From supplier DC Chemicals

Cas No.:	658084-23-2
Chemical Name:	(Z)-N-(3-chlorophenyl)-3-((3,5-dimethyl-4-(1-methylpiperazine-4-carbonyl)-1H-pyrrol-2-yl)methylene)-N-methyl-2-oxoindoline-5-sulfonamide
Synonyms:	SU-11274,PKI-SU11274,SU 11274
SMILES:	N1C2=C(C=C(S(N(C3=CC=CC(Cl)=C3)C)(=O)=O)C=C2)/C(=C/C2=C(C)C(C(N3CCN(C)CC3)=O)=C(C)N2)/C1=O
Formula:	C₂₈H₃₀CIn₅O₄S
M.Wt:	568.09
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

SU11274 is a selective Met inhibitor with IC50 of 10 nM, but has no effects on PGDFRβ, EGFR or Tie2.

In Vitro:

SU11274 exhibits greater than 50-fold selectivity for Met versus Flk and more than 500 times selectivity versus other tyrosine kinases such as FGFR-1, c-src, PDGFbR, and EGFR. SU11274 inhibits the phosphorylation of key regulators of the PI3K pathway, including AKT, FKHR, or GSK3β. SU11274 treatment inhibits the growth of TPR-MET-transformed BaF3 cells in a dose-dependent manner with IC50 of < 3 μM in the absence of interleukin 3, without growth inhibition of BaF3 cells transformed by other oncogenic tyrosine kinases, including BCR-ABL, TEL-JAK2, TEL-ABL, and TEL-PDGFβR. In addition to cell growth, SU11274 treatment significantly inhibits the migration of BaF3. TPR-MET cells by 44.8% and 80% at 1 μM and 5 μM, respectively. SU11274 inhibits HGF-dependent phosphorylation of Met as well as HGF-dependent cell proliferation and motility with an IC50 of 1-1.5 μM. In H69 and H345 cells which have functional Met receptor, SU11274 inhibits the HGF-induced cell growth with IC50 of 3.4 μM and 6.5 μM, respectively. SU11274 induces G1 cell cycle arrest with cells in G1 phase increased from 42.4% to 70.6% at 5 μM, and induces caspase-dependent apoptosis by 24% at 1 μM[2]. SU11274 inhibits cell viability in c-Met-expressing non-small cell lung cancer (NSCLC) cells with IC50 values of 0.8-4.4 μM, and abrogates hepatocyte growth factor-induced phosphorylation of c-Met and its downstream signaling[3].

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC7065	Tivantinib (ARQ 197)	Tivantinib (ARQ 197) is the first non-ATP-competitive c-Met inhibitor with Ki of 0.355 μM, little activity to Ron, and no inhibition to EGFR, InsR, PDGFRα or FGFR1/4.
DC1093	SU11274 (PKI-SU11274)	SU11274 is a selective Met inhibitor with IC50 of 10 nM.
DC7672	SAR125844	SAR125844 is inhibitor of the proto-oncogene c-Met (also known as hepatocyte growth factor receptor [HGFR]) with potential antineoplastic activity.
DC7081	PF-04217903	PF-04217903 is a selective ATP-competitive c-Met inhibitor with IC50 of 4.8 nM, susceptible to oncogenic mutations (no activity to Y1230C mutant).
DC7177	JNJ 38877605	JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases.
DC7167	Capmatinib(INCB28060)	INCB28060 is a novel orally active inhibitor (IC50=0.13 nM) of c-MET kinase.
DC5065	Golvatinib (E7050)	E-7050 is hepatocyte growth factor receptors (HGFR).
DC8845	AMG337	AMG-337 is a potent and highly selective small molecule ATP-competitive MET kinase inhibitor. AMG 337 inhibits MET kinase activity with an IC50 of < 5nM in enzymatic assays.
DC7056	AMG-208	AMG-208 is a potent small molecular c-Met inhibitor with an IC50 of 9.3 nM.

SU11274 (PKI-SU11274)