JNJ-38877605

Validation & Quality Control

Product Citations(4)

PLoS Biol, 2011, 9(9), e1001162

Neoplasia, 2011, 13(12), 1132-1142

Brit J Cancer, 2011, 105(3), 382-392

PLoS One, 2012, 7(9):e44937

Customer Reviews(5) in vivo invitation

Quality Control & MSDS

Related Compound Libraries

JNJ-38877605 is available in the following compound libraries:

Inhibitor Library (96-well) Kinase Inhibitor Library (96-well) Chemical Library (96-well) Tyrosine Kinase Inhibitor Library (96-Well) Cambridge Cancer Compound Library(96-well)

Product Information

Compare c-Met Inhibitors

Research Area
Research Area
Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

Cat.No.	Product Name	Solubility (25°C)
S1068	Crizotinib (PF-02341066)	<1 mg/mL	20 mg/mL	<1 mg/mL
S1119	XL-184 free base (Cabozantinib)	<1 mg/mL	100 mg/mL	<1 mg/mL
S1111	Foretinib (GSK1363089, XL880)	<1 mg/mL	127 mg/mL	<1 mg/mL
S1070	PHA-665752	<1 mg/mL	128 mg/mL	<1 mg/mL
S1080	SU11274	<1 mg/mL	92 mg/mL	2 mg/mL
S1094	PF-04217903	<1 mg/mL	5 mg/mL	<1 mg/mL
S1112	SGX-523	<1 mg/mL	2 mg/mL	<1 mg/mL
S1561	BMS 777607	<1 mg/mL	47 mg/mL	<1 mg/mL
S2753	ARQ 197 (Tivantinib)	<1 mg/mL	74 mg/mL	40 mg/mL
S1114	JNJ-38877605	<1 mg/mL	37 mg/mL	<1 mg/mL
S2788	INCB28060	<1 mg/mL	2 mg/mL	<1 mg/mL
S1361	MGCD-265	<1 mg/mL	104 mg/mL	<1 mg/mL
S2774	MK-2461	<1 mg/mL	99 mg/mL	<1 mg/mL
S1316	AMG-208	<1 mg/mL	0.25 mg/mL	<1 mg/mL
S2859	Golvatinib (E7050)	<1 mg/mL	20 mg/mL	<1 mg/mL
S2747	AMG458	<1 mg/mL	21 mg/mL	<1 mg/mL
S2201	BMS 794833	<1 mg/mL	94 mg/mL	<1 mg/mL
S2761	NVP-BVU972	<1 mg/mL	68 mg/mL	68 mg/mL

Product Description

Biological Activity Protocol Chemical Information Customer Reviews Product Citations Tech Support & FAQs

Biological Activity

Description	JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM.
Targets	c-Met
IC50	4 nM ^[1]
In vitro	JNJ-38877605 shows more than 600-fold selectivity for c-Met compared with more than 200 other diverse tyrosine and serine-threonine kinases and also potently inhibits HGF-stimulated and constitutively activated c-Met phosphorylation in vitro. ^[1] In EBC1, GTL16, NCI-H1993, and MKN45 cells, JNJ-38877605 (500 nM) leads to a significant reduction of phosphorylation of Met and RON, another key player in invasive growth. ^[2] A recent study shows that JNJ-38877605 is involved in modulating secretion of IL-8, GROa, uPAR and IL-6 in GTL16 cells. ^[3]
In vivo	In mice bearing established GTL16 xenografts, JNJ-38877605, dosed orally with 40 mg/kg/day for 72 hours, results in a statistically significant decrease in the plasma levels of human IL-8 (from 0.150 ng/mL to 0.050 ng/mL) and GROα (from 0.080 ng/mL to 0.030 ng/mL). While concentrations of uPAR in the blood become reduced to more than 50% at the same dose. ^[3]
Clinical Trials	JNJ-38877605 is currently in Phase I clinical trials in patients with Neoplasms.
Features

Protocol(Only for Reference)

Animal Study: ^[3]

Animal Models	GTL16 cells are inoculated subcutaneously into the right posterior flank (or both right and left posterior flanks, for determination of uPAR and IL-6) of 6-week-old immunodeficient nu/nu female mice on Swiss CD1 background.
Formulation	JNJ-38877605 is dissolved in PBS.
Dosages	≤40 mg/kg/day
Administration	Administered via p.o.

1

References

Chemical Information

Download JNJ-38877605 SDF

Molecular Weight (MW)	377.35
Formula	C₁₉H₁₃F₂N₇
CAS No.	943540-75-8, 1093204-17-1 (X methanesulfonate), 1093204-20-6 (XHCl)
Synonyms	N/A

Solubility (25°C) DMSO 37 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
Storage	2 years -20°CPowder
	2 weeks4°Cin DMSO
	6 months-80°Cin DMSO

Chemical Name	6-(difluoro(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl)quinoline

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Research Area

Customer Reviews (5)

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Rating

Source

PLOS one, 2012. 7(9), e44937. JNJ-38877605 purchased from Selleck

Method

Western Blot

Cell Lines

RPE50 cells

Concentrations

Incubation Time

0.5 h

Results

Click to enlarge

Rating

Source

PLOS one, 2012. 7(9), e44937. JNJ-38877605 purchased from Selleck

Method

Wound healing assay

Cell Lines

RPE50 and ARPE19 cells

Concentrations

Incubation Time

18 h

Results

As positive controls, JNJ38877605 and AG1478, theinhibitors of c-met (the receptor of HGF) and EGFR (the receptorof both EGF and HB-EGF) abolished migration of both types of RPE cells induced by HGF and EGF, respectively.

Click to enlarge

Rating

Source

PLoS One, 2012, 7(9), e44937.. JNJ-38877605 purchased from Selleck

Method

Western blot

Cell Lines

RPE50 cells

Concentrations

50 nM

Incubation Time

0.5 h

Results

HGF-induced phosphorylation of ERK at 0.5 h can be reduced by BIS, PD98059 and JNJ38877605 by 70, 58 and 77%Respectively.

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Rating

Source

PLoS Biol , 2011, 9, e1001162 . JNJ-38877605 purchased from Selleck

Method

qRT-PCR, Immunofluorescence

Cell Lines

RETAAD tumor cells, NBT-II cells, PMN-MDSCs

Concentrations

Incubation Time

24 h

Results

We found that JNJ-38877605 and other inhibitors of the corresponding receptors blocked PMN-MDSC mediated induction of EMT. The fact that EGF inhibitors reduced EMT induction while PMN-MDSC purified from RETAAD tumors did not produce EGF may suggest that PMN-MDSC stimulate EGF production by the cancer cells.

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Rating

Source

Dr. Zhang of Tianjin Medical University. JNJ-38877605 purchased from Selleck

Method

Western blot

Cell Lines

Breast cancer cells

Concentrations

0-1000 nM

Incubation Time

3 h

Results

JNJ-38877605 treatment resulted in a reduction of c-Met phosphorylation in Breast cancer cells.

Product Citations (4)

Mesenchymal transition and dissemination of cancer cells is driven by myeloid-derived suppressor cells infiltrating the primary tumor. [Toh B, et al. PLoS Biol 2011;9(9), e1001162]
PubMed: 21980263
Identification of MET and SRC activation in melanoma cell lines showing primary resistance to PLX4032. [Vergani E, et al. Neoplasia 2011;13(12), 1132-1142]
PubMed: 22241959
Antitumour efficacy of MEK inhibitors in human lung cancer cells and their derivatives with acquired resistance to different tyrosine kinase inhibitors. [Morgillo F, et al. Brit J Cancer 2011;105(3), 382-392]
PubMed: 21750552

Enhanced PKCδ and ERK Signaling Mediate Cell Migration of Retinal Pigment Epithelial Cells Synergistically Induced by HGF and EGF. [Chen YJ, et al. PLoS One 2012;7(9):e44937]
PubMed: 23028692

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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PHA-665752 is a potent, selective and ATP-competitive c-Met inhibitor with IC50 of 9 nM.
SU11274

SU11274 is a selective Met inhibitor with IC50 of 10 nM.
PF-04217903

PF-04217903 is a selective ATP-competitive c-Met inhibitor with IC50 of 4.8 nM.
Foretinib (GSK1363089, XL880)

XL880 (GSK1363089, EXEL-2880) is an ATP-competitive inhibitor of MET and KDR with IC50 of 0.4 nM and 0.9 nM, respectively.
SGX-523

SGX-523 is a selective Met inhibitor with IC50 of 4 nM.
AMG-208
AMG-208 is a highly selective c-Met inhibitor with IC50 of 9.3 nM.
MGCD-265

MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met, VEGFR1, VEGFR2, VEGFR3, Ron, and Tie2 with IC50 of 1 nM, 3 nM, 3 nM, 4 nM, 2 nM and 7 nM, respectively.
BMS 777607

BMS-777607 is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50 of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively.
BMS 794833
BMS794833 is a potent ATP competitive inhibitor of Met and VEGFR2 with IC50 of 1.7 nM and 15 nM, respectively.
AMG458
AMG 458 is a potent c-Met inhibitor of human c-Met and mouse c-Met with K_i of 1.2 nM or 2.0 nM.

RTKs and Angiogenesis Related Products

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Product Categories

Validation & Quality Control

Product Citations(4)

Customer Reviews(5) in vivo invitation

Quality Control & MSDS

Related Compound Libraries

JNJ-38877605 is available in the following compound libraries:

Product Information

Compare c-Met Inhibitors

Research Area

Product Description

Biological Activity

Protocol(Only for Reference)

Animal Study: ^[3]

References

Chemical Information

Research Area

Customer Reviews (5)

Product Citations (4)

Tech Support & FAQs

If you have any other enquiries, please leave a message.

Related c-Met Inhibitors

RTKs and Angiogenesis Related Products

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Product Categories

JNJ-38877605

Validation & Quality Control

Product Citations(4)

Customer Reviews(5) in vivo invitation

Quality Control & MSDS

Related Compound Libraries

JNJ-38877605 is available in the following compound libraries:

Product Information

Compare c-Met Inhibitors

Research Area

Product Description

Biological Activity

Protocol(Only for Reference)

Animal Study: [3]

References

Chemical Information

Research Area

Customer Reviews (5)

Product Citations (4)

Tech Support & FAQs

If you have any other enquiries, please leave a message.

Related c-Met Inhibitors

RTKs and Angiogenesis Related Products

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Animal Study: ^[3]