SU11274

SKU: orb1224320

Description

SU11274 (PKI-SU11274) is a potent, selective, ATP-competitive c-Met kinase inhibitor with IC50 of 20 nM, >50-fold selectivity over Bcr-Abl, JAK2, PDGFβR; induces G(1) cell cycle arrest and apoptosis with increased Annexin V staining and caspase 3 activity, specifically regulates cell growth in TPR-MET-transformed BaF3 cells with IC50 of <3 uM, differentially affects the kinase activity and subsequent signaling of various mutant forms of Met (M1268T and H1112Y).

Images & Validation

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Key Properties

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CAS Number	658084-23-2
MW	568.0869
Purity	>98% (HPLC)
Formula	C₂₈H₃₀ClN₅O₄S
SMILES	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
Target	c-Met/HGFR
Solubility	10 mM in DMSO

Bioactivity

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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. 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.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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SU 11274 | PKI-SU11274 | SU-11274

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Gene Symbol

c-Met/HGFR

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SU11274 (orb1224320)

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Purity:	99.44%
CAS Number:	658084-23-2
MW:	568.09
Formula:	C₂₈H₃₀ClN₅O₄S

SU11274

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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