Grouped product items

SKU

Size

Availability

Price

Qty

T127502-5mg

5mg

In stock

$39.90

T127502-10mg

10mg

In stock

$69.90

T127502-25mg

25mg

In stock

$129.90

T127502-50mg

50mg

In stock

$199.90

T127502-100mg

100mg

In stock

$299.90

T127502-250mg

250mg

In stock

$659.90

Basic Description

Synonyms	Tivantinib\|905854-02-6\|ARQ-197\|ARQ 197\|(3R,4R)-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione\|Tivantinib (ARQ 197)\|ARQ197\|905853-99-8\|1000873-98-2\|rel-(3R,4R)-3-(5,6-Dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1
Specifications & Purity	Moligand™, ≥98%
Biochemical and Physiological Mechanisms	Tivantinib is an orally available, small molecule inhibitor of the c-Met receptor tyrosine kinase.
Storage Temp	Store at -20°C,Argon charged
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Hepatocyte growth factor receptor inhibitor

Product Properties

ALogP	2.9

Associated Targets

CTDNEP1 Tbio CTD nuclear envelope phosphatase 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK1 Tchem Cyclin-dependent kinase 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

EPHB6 Tchem Ephrin type-B receptor 6 0 Activities

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EGFR Tclin Epidermal growth factor receptor 0 Activities

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DNAJA1 Tchem DnaJ homolog subfamily A member 1 0 Activities

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CDK9 Tchem Cyclin-dependent kinase 9 0 Activities

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CDK16 Tchem Cyclin-dependent kinase 16 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK4 Tclin Cyclin-dependent kinase 4 0 Activities

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CDK17 Tchem Cyclin-dependent kinase 17 0 Activities

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CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

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CDK5 Tchem Cyclin-dependent-like kinase 5 0 Activities

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SRC Tclin Proto-oncogene tyrosine-protein kinase Src 0 Activities

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YES1 Tclin Tyrosine-protein kinase Yes 0 Activities

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TYK2 Tclin Non-receptor tyrosine-protein kinase TYK2 0 Activities

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HDAC6 Tclin Histone deacetylase 6 0 Activities

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FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 0 Activities

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FGFR1 Tclin Fibroblast growth factor receptor 1 0 Activities

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MET Tclin Hepatocyte growth factor receptor 1 Activities

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IGF1R Tclin Insulin-like growth factor 1 receptor 0 Activities

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SIK2 Tchem Serine/threonine-protein kinase SIK2 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PLK4 Tchem Serine/threonine-protein kinase PLK4 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PIM1 Tchem Serine/threonine-protein kinase pim-1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PIM2 Tchem Serine/threonine-protein kinase pim-2 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDGFRB Tclin Platelet-derived growth factor receptor beta 0 Activities

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MCM4 Tchem DNA replication licensing factor MCM4 0 Activities

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MAP2K2 Tclin Dual specificity mitogen-activated protein kinase kinase 2 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAP4K5 Tchem Mitogen-activated protein kinase kinase kinase kinase 5 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BMPR1B Tchem Bone morphogenetic protein receptor type-1B 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BTK Tclin Tyrosine-protein kinase BTK 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AURKA Tchem Aurora kinase A 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AURKB Tchem Aurora kinase B 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AAK1 Tchem AP2-associated protein kinase 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TNK2 Tclin Activated CDC42 kinase 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ACAD10 Tchem Acyl-CoA dehydrogenase family member 10 0 Activities

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ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

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AKT3 Tchem RAC-gamma serine/threonine-protein kinase 0 Activities

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AKT2 Tchem RAC-beta serine/threonine-protein kinase 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AKT1 Tchem RAC-alpha serine/threonine-protein kinase 0 Activities

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CHEK1 Tchem Serine/threonine-protein kinase Chk1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CLK3 Tchem Dual specificity protein kinase CLK3 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CLK1 Tchem Dual specificity protein kinase CLK1 0 Activities

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CLK2 Tchem Dual specificity protein kinase CLK2 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CLK4 Tchem Dual specificity protein kinase CLK4 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GSK3A Tclin Glycogen synthase kinase-3 alpha 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NTRK1 Tclin High affinity nerve growth factor receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAP2K1 Tclin Dual specificity mitogen-activated protein kinase kinase 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

Pubchem Sid	488197553
Pubchem Sid Url	https://pubchem.ncbi.nlm.nih.gov/substance/488197553
IUPAC Name	(3R,4R)-3-(1-azatricyclo[6.3.1.04,12]dodeca-2,4,6,8(12)-tetraen-3-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione
INCHI	InChI=1S/C23H19N3O2/c27-22-19(16-11-24-18-9-2-1-7-14(16)18)20(23(28)25-22)17-12-26-10-4-6-13-5-3-8-15(17)21(13)26/h1-3,5,7-9,11-12,19-20,24H,4,6,10H2,(H,25,27,28)/t19-,20-/m0/s1
InChi Key	UCEQXRCJXIVODC-PMACEKPBSA-N
Canonical SMILES	C1CC2=C3C(=CC=C2)C(=CN3C1)C4C(C(=O)NC4=O)C5=CNC6=CC=CC=C65
Isomeric SMILES	C1CC2=C3C(=CC=C2)C(=CN3C1)[C@H]4[C@@H](C(=O)NC4=O)C5=CNC6=CC=CC=C65
PubChem CID	11494412
Molecular Weight	369.42

Database links

PubChem SID	488197553

Certificates

Certificate of Analysis(COA)

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19 results found

Lot Number	Certificate Type	Date	Item
A2411392	Certificate of Analysis	Dec 16, 2023	T127502
A2411375	Certificate of Analysis	Dec 16, 2023	T127502
A2411374	Certificate of Analysis	Dec 16, 2023	T127502
A2411373	Certificate of Analysis	Dec 16, 2023	T127502
A2219439	Certificate of Analysis	Nov 10, 2023	T127502
A2219743	Certificate of Analysis	Nov 10, 2023	T127502
A2219695	Certificate of Analysis	Nov 10, 2023	T127502
A2219435	Certificate of Analysis	Nov 10, 2023	T127502
C23241005	Certificate of Analysis	Feb 03, 2023	T127502
C23241009	Certificate of Analysis	Feb 03, 2023	T127502
C23241010	Certificate of Analysis	Feb 03, 2023	T127502
C23241011	Certificate of Analysis	Feb 03, 2023	T127502
C23241018	Certificate of Analysis	Feb 03, 2023	T127502
C23241124	Certificate of Analysis	Feb 03, 2023	T127502
C2324973	Certificate of Analysis	Feb 03, 2023	T127502
C2324976	Certificate of Analysis	Feb 03, 2023	T127502
C2324979	Certificate of Analysis	Feb 03, 2023	T127502
A2219742	Certificate of Analysis	Jan 04, 2022	T127502
A2219696	Certificate of Analysis	Jan 04, 2022	T127502

Chemical and Physical Properties

Solubility	DMSO 74 mg/mL Water <1 mg/mL Ethanol 40 mg/mL

Safety and Hazards(GHS)

Pictogram(s)	GHS08
Signal	Danger
Hazard Statements	H373:Causes damage to organs through prolonged or repeated exposure H360:May damage fertility or the unborn child
Precautionary Statements	P280:Wear protective gloves/protective clothing/eye protection/face protection. P405:Store locked up. P501:Dispose of contents/container to ... P260:Do not breathe dust/fume/gas/mist/vapors/spray. P203:Obtain, read and follow all safety instructions before use. P318:if exposed or concerned, get medical advice. P319:Get medical help if you feel unwell.

References

1. Danilkovitch-Miagkova A, Zbar B. (2002) Dysregulation of Met receptor tyrosine kinase activity in invasive tumors.. J Clin Invest, 109 (7): (863-7). [PMID:11927612]
2. Birchmeier C, Birchmeier W, Gherardi E, Vande Woude GF. (2003) Met, metastasis, motility and more.. Nat Rev Mol Cell Biol, 4 (12): (915-25). [PMID:14685170]
3. Boccaccio C, Comoglio PM. (2006) Invasive growth: a MET-driven genetic programme for cancer and stem cells.. Nat Rev Cancer, 6 (8): (637-45). [PMID:16862193]
4. Munshi N, Jeay S, Li Y, Chen CR, France DS, Ashwell MA, Hill J, Moussa MM, Leggett DS, Li CJ. (2010) ARQ 197, a novel and selective inhibitor of the human c-Met receptor tyrosine kinase with antitumor activity.. Mol Cancer Ther, 9 (6): (1544-53). [PMID:20484018]
5. Sequist LV, von Pawel J, Garmey EG, Akerley WL, Brugger W, Ferrari D, Chen Y, Costa DB, Gerber DE, Orlov S et al.. (2011) Randomized phase II study of erlotinib plus tivantinib versus erlotinib plus placebo in previously treated non-small-cell lung cancer.. J Clin Oncol, 29 (24): (3307-15). [PMID:21768463]
6. Katayama R, Aoyama A, Yamori T, Qi J, Oh-hara T, Song Y, Engelman JA, Fujita N. (2013) Cytotoxic activity of tivantinib (ARQ 197) is not due solely to c-MET inhibition.. Cancer Res, 73 (10): (3087-96). [PMID:23598276]
7. Rimassa L, Bruix J, Broggini M, Santoro A. (2013) Tivantinib (ARQ197) displays cytotoxic activity that is independent of its ability to bind MET--letter.. Clin Cancer Res, 19 (15): (4290). [PMID:23766362]

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Tivantinib (ARQ 197) - 98%, high purity , Hepatocyte growth factor receptor inhibitor, CAS No.905854-02-6, Hepatocyte growth factor receptor inhibitor

Basic Description

Product Properties

Associated Targets

CTDNEP1 Tbio CTD nuclear envelope phosphatase 1 0 Activities

CDK1 Tchem Cyclin-dependent kinase 1 0 Activities

EPHB6 Tchem Ephrin type-B receptor 6 0 Activities

EGFR Tclin Epidermal growth factor receptor 0 Activities

DNAJA1 Tchem DnaJ homolog subfamily A member 1 0 Activities

CDK9 Tchem Cyclin-dependent kinase 9 0 Activities

CDK16 Tchem Cyclin-dependent kinase 16 0 Activities

CDK4 Tclin Cyclin-dependent kinase 4 0 Activities

CDK17 Tchem Cyclin-dependent kinase 17 0 Activities

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

CDK5 Tchem Cyclin-dependent-like kinase 5 0 Activities

SRC Tclin Proto-oncogene tyrosine-protein kinase Src 0 Activities

YES1 Tclin Tyrosine-protein kinase Yes 0 Activities

TYK2 Tclin Non-receptor tyrosine-protein kinase TYK2 0 Activities

HDAC6 Tclin Histone deacetylase 6 0 Activities

FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 0 Activities

FGFR1 Tclin Fibroblast growth factor receptor 1 0 Activities

MET Tclin Hepatocyte growth factor receptor 1 Activities

IGF1R Tclin Insulin-like growth factor 1 receptor 0 Activities

SIK2 Tchem Serine/threonine-protein kinase SIK2 0 Activities

PLK4 Tchem Serine/threonine-protein kinase PLK4 0 Activities

PIM1 Tchem Serine/threonine-protein kinase pim-1 0 Activities

PIM2 Tchem Serine/threonine-protein kinase pim-2 0 Activities

PDGFRB Tclin Platelet-derived growth factor receptor beta 0 Activities

MCM4 Tchem DNA replication licensing factor MCM4 0 Activities

MAP2K2 Tclin Dual specificity mitogen-activated protein kinase kinase 2 0 Activities

MAP4K5 Tchem Mitogen-activated protein kinase kinase kinase kinase 5 0 Activities

BMPR1B Tchem Bone morphogenetic protein receptor type-1B 0 Activities

BTK Tclin Tyrosine-protein kinase BTK 0 Activities

AURKA Tchem Aurora kinase A 0 Activities

AURKB Tchem Aurora kinase B 0 Activities

AAK1 Tchem AP2-associated protein kinase 1 0 Activities

TNK2 Tclin Activated CDC42 kinase 1 0 Activities

ACAD10 Tchem Acyl-CoA dehydrogenase family member 10 0 Activities

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

AKT3 Tchem RAC-gamma serine/threonine-protein kinase 0 Activities

AKT2 Tchem RAC-beta serine/threonine-protein kinase 0 Activities

AKT1 Tchem RAC-alpha serine/threonine-protein kinase 0 Activities

CHEK1 Tchem Serine/threonine-protein kinase Chk1 0 Activities

CLK3 Tchem Dual specificity protein kinase CLK3 0 Activities

CLK1 Tchem Dual specificity protein kinase CLK1 0 Activities

CLK2 Tchem Dual specificity protein kinase CLK2 0 Activities

CLK4 Tchem Dual specificity protein kinase CLK4 0 Activities

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

GSK3A Tclin Glycogen synthase kinase-3 alpha 0 Activities

NTRK1 Tclin High affinity nerve growth factor receptor 0 Activities

MAP2K1 Tclin Dual specificity mitogen-activated protein kinase kinase 1 0 Activities

Names and Identifiers

Database links

Certificates

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Chemical and Physical Properties

Safety and Hazards(GHS)

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References

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