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Defactinib - ≥98%, high purity , CAS No.1073154-85-4

Moligand™
≥98%

CAS#: 1073154-85-4
Formula: C₂₀H₂₁F₃N₈O₃S
Molecular Weight: 510.49
PubChem CID: 25117126

Item Number

D275494

Grouped product items
SKU	Size	Availability	Price
D275494-5mg	5mg	In stock	$82.90
D275494-10mg	10mg	In stock	$105.90
D275494-25mg	25mg	In stock	$238.90
D275494-50mg	50mg	In stock	$296.90
D275494-100mg	100mg	In stock	$414.90
D275494-250mg	250mg	In stock	$933.90

Potent FAK inhibitor

Basic Description

Synonyms	Defactinib\|1073154-85-4\|PF-04554878\|VS-6063\|1345713-71-4\|Defactinib (VS-6063, PF-04554878)\|N-methyl-4-((4-(((3-(N-methylmethylsulfonamido)pyrazin-2-yl)methyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)benzamide\|N-methyl-4-[[4-[[3-[methyl(methylsulfony
Specifications & Purity	≥98%
Storage Temp	Store at -20°C,Desiccated
Shipped In	Dry ice
Grade	Moligand™
Product Description	Shipped at Room Temperature. Store at -20°C. Store under desiccating conditions.

Associated Targets

PTK2 Tclin Focal adhesion kinase 1 5 Activities

Discover Target: PTK2

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

CDKL5 Tchem Cyclin-dependent kinase-like 5 1 Activities

Discover Target: CDKL5

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

NTRK1 Tclin High affinity nerve growth factor receptor 1 Activities

Discover Target: NTRK1

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

JAK2 Tclin Tyrosine-protein kinase JAK2 1 Activities

Discover Target: JAK2

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

Names and Identifiers

IUPAC Name	N-methyl-4-[[4-[[3-[methyl(methylsulfonyl)amino]pyrazin-2-yl]methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]amino]benzamide
INCHI	InChI=1S/C20H21F3N8O3S/c1-24-18(32)12-4-6-13(7-5-12)29-19-28-10-14(20(21,22)23)16(30-19)27-11-15-17(26-9-8-25-15)31(2)35(3,33)34/h4-10H,11H2,1-3H3,(H,24,32)(H2,27,28,29,30)
InChi Key	FWLMVFUGMHIOAA-UHFFFAOYSA-N
Canonical SMILES	CNC(=O)C1=CC=C(C=C1)NC2=NC=C(C(=N2)NCC3=NC=CN=C3N(C)S(=O)(=O)C)C(F)(F)F
Isomeric SMILES	CNC(=O)C1=CC=C(C=C1)NC2=NC=C(C(=N2)NCC3=NC=CN=C3N(C)S(=O)(=O)C)C(F)(F)F
Alternate CAS	1073154-85-4
PubChem CID	25117126
MeSH Entry Terms	defactinib;N-methyl-4-((4-(((3-methyl(methylsulfonyl)aminopyrazin-2-yl)methyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)benzamide;PF-04554878;VS-6063
Molecular Weight	510.49

Certificates

Certificate of Analysis(COA)

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11 results found

Lot Number	Certificate Type	Date	Item
I2227383	Certificate of Analysis	Jul 13, 2023	D275494
I2227385	Certificate of Analysis	Jul 13, 2023	D275494
I2227386	Certificate of Analysis	Jul 13, 2023	D275494
I2227387	Certificate of Analysis	Jul 13, 2023	D275494
I2227388	Certificate of Analysis	Jul 13, 2023	D275494
I2227389	Certificate of Analysis	Jul 13, 2023	D275494
L2109097	Certificate of Analysis	Jun 14, 2023	D275494
L2108516	Certificate of Analysis	Sep 13, 2022	D275494
L2108518	Certificate of Analysis	Sep 13, 2022	D275494
L2109098	Certificate of Analysis	Sep 13, 2022	D275494
L2109099	Certificate of Analysis	Sep 13, 2022	D275494

Safety and Hazards(GHS)

Pictogram(s)	GHS07
Signal	Warning
Hazard Statements	H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation H302:Harmful if swallowed
Precautionary Statements	P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing.

References

1. Golubovskaya VM, Cance WG. (2007) Focal adhesion kinase and p53 signaling in cancer cells.. Int Rev Cytol, 263 (3): (103-53). [PMID:17725966]
2. Provenzano PP, Keely PJ. (2009) The role of focal adhesion kinase in tumor initiation and progression.. Cell Adh Migr, 3 (4): (347-50). [PMID:19690467]
3. Kang Y, Hu W, Ivan C, Dalton HJ, Miyake T, Pecot CV, Zand B, Liu T, Huang J, Jennings NB et al.. (2013) Role of focal adhesion kinase in regulating YB-1-mediated paclitaxel resistance in ovarian cancer.. J Natl Cancer Inst, 105 (19): (1485-95). [PMID:24062525]
4. Jones SF, Siu LL, Bendell JC, Cleary JM, Razak AR, Infante JR, Pandya SS, Bedard PL, Pierce KJ, Houk B et al.. (2015) A phase I study of VS-6063, a second-generation focal adhesion kinase inhibitor, in patients with advanced solid tumors.. Invest New Drugs, 33 (5): (1100-7). [PMID:26334219]
5. Shimizu T, Fukuoka K, Takeda M, Iwasa T, Yoshida T, Horobin J, Keegan M, Vaickus L, Chavan A, Padval M et al.. (2016) A first-in-Asian phase 1 study to evaluate safety, pharmacokinetics and clinical activity of VS-6063, a focal adhesion kinase (FAK) inhibitor in Japanese patients with advanced solid tumors.. Cancer Chemother Pharmacol, 77 (5): (997-1003). [PMID:27025608]
6. Lin HM, Lee BY, Castillo L, Spielman C, Grogan J, Yeung NK, Kench JG, Stricker PD, Haynes AM, Centenera MM et al.. (2018) Effect of FAK inhibitor VS-6063 (defactinib) on docetaxel efficacy in prostate cancer.. Prostate, 78 (4): (308-317). [PMID:29314097]
7. Polte TR, Hanks SK. (1995) Interaction between focal adhesion kinase and Crk-associated tyrosine kinase substrate p130Cas.. Proc Natl Acad Sci USA, 92 (23): (10678-82). [PMID:7479864]
8. Schaller MD, Hildebrand JD, Shannon JD, Fox JW, Vines RR, Parsons JT. (1994) Autophosphorylation of the focal adhesion kinase, pp125FAK, directs SH2-dependent binding of pp60src.. Mol Cell Biol, 14 (3): (1680-8). [PMID:7509446]
9. Owens LV, Xu L, Dent GA, Yang X, Sturge GC, Craven RJ, Cance WG. (1996) Focal adhesion kinase as a marker of invasive potential in differentiated human thyroid cancer.. Ann Surg Oncol, 3 (1): (100-5). [PMID:8770310]

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