ChemicalBook > CAS DataBase List > Defactinib

Defactinib

Product Name: Defactinib
CAS No.: 1073154-85-4
Chemical Name: Defactinib
Synonyms: VS6063;VS-6063;VS 6063;CS-1796;PF-941222;Defactinib;Defactinib (VS-6063;VS-6063; PF-04554878;Defactinib free base;PF-04554878 Defactinib
CBNumber: CB82716190
Molecular Formula: C20H21F3N8O3S
Formula Weight: 510.49
MOL File: 1073154-85-4.mol

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Defactinib Property

Density: 1.495±0.06 g/cm3(Predicted)
storage temp.: -20°C (des.)
solubility: Soluble in DMSO (up to at least 25mg/ml)
form: solid
pka: 15.16±0.46(Predicted)
color: White
Stability:: Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
InChIKey: FWLMVFUGMHIOAA-UHFFFAOYSA-N
SMILES: C(NC)(=O)C1=CC=C(NC2=NC=C(C(F)(F)F)C(NCC3=NC=CN=C3N(C)S(C)(=O)=O)=N2)C=C1

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word: Warning

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 17737
Product name: Defactinib
Purity: ≥98%
Packaging: 1mg
Price: $37
Updated: 2024/03/01

Cayman Chemical

Product number: 17737
Product name: Defactinib
Purity: ≥98%
Packaging: 5mg
Price: $116
Updated: 2024/03/01

Cayman Chemical

Product number: 17737
Product name: Defactinib
Purity: ≥98%
Packaging: 10mg
Price: $213
Updated: 2024/03/01

Cayman Chemical

Product number: 17737
Product name: Defactinib
Purity: ≥98%
Packaging: 25mg
Price: $353
Updated: 2024/03/01

Usbiological

Product number: 474093
Product name: Defactinib
Packaging: 100mg
Price: $1380
Updated: 2021/12/16

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Defactinib Chemical Properties,Usage,Production

Description

Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase that plays a vital role in many oncogenic pathways. Defactinib is a dose-dependent inhibitor of FAK, with maximal inhibition of FAK autophosphorylation in cells achieved at 10 μM. It is less effective against the related kinase PYK2. Defactinib restores the chemosensitivity of taxane-resistant cells to paclitaxel , although it is not cytotoxic alone. Defactinib decreases YB-1 phosphorylation and nuclear accumulation in an Akt-dependent manner. It is orally bioavailable, inhibiting FAK and augmenting paclitaxel action in suppressing the growth and number of ovarian cancer cell tumors in mice.

Uses

Defactinib is a selective and orally active FAK inhibitor phase 2. Used in treating cancer patients as it decreases proliferation and increases apoptosis.

in vivo

Defactinib (VS-6063) doses of 25 mg/kg twice a day or greater statistically significantly inhibits pFAK (Tyr397) at 3 hours, with return of expression noted by 24 hours. Therefore, administration of Defactinib at 25 mg/kg twice a day is selected as the dosing schedule for subsequent therapy experiments. For therapy experiments, female nude mice bearing HeyA8 tumors in the peritoneal cavity are randomly divided into 4 groups (n=10 per group): 1) vehicle orally twice daily and phosphate-buffered saline intraperitoneally weekly (control); 2) Defactinib 25 mg/kg orally twice daily; 3) PTX intraperitoneally weekly; and 4) both VDefactinib 25 mg/kg orally twice daily and PTX intraperitoneally weekly. There is an 87.4% reduction in tumor weight by PTX monotherapy in the HeyA8 model, and combination therapy resulted in the greatest tumor weight reduction, with a 97.9% reduction (P=0.05 compared with PTX). In the SKOV3ip1 model, a 92.7% tumor weight reduction is observed in the combination group compared with PTX (P<0.001)^[1].

storage

Store at -20°C

References

[1] SUZANNE F JONES. A phase I study of VS-6063, a second-generation focal adhesion kinase inhibitor, in patients with advanced solid tumors.[J]. Investigational New Drugs, 2015, 33 5: 1100-1107. DOI:10.1007/s10637-015-0282-y
[2] VIHREN N KOLEV. Inhibition of FAK kinase activity preferentially targets cancer stem cells.[J]. Oncotarget, 2017: 51733-51747. DOI:10.18632/oncotarget.18517
[3] FABRIZIO MARCUCCI François L Cristiano Rumio. Anti-Cancer Stem-like Cell Compounds in Clinical Development - An Overview and Critical Appraisal.[J]. Frontiers in Oncology, 2016: 115. DOI:10.3389/fonc.2016.00115
[4] J. RING. FAK/PYK2 inhibitors defactinib and VS-4718 enhance immune checkpoint inhibitor efficacy[J]. Journal for Immunotherapy of Cancer, 2015, 3 1: P354-P354. DOI:10.1186/2051-1426-3-s2-p354
[5] HONG JIANG. Targeting focal adhesion kinase renders pancreatic cancers responsive to checkpoint immunotherapy[J]. Nature Medicine, 2016, 22 8: 851-860. DOI:10.1038/nm.4123

Defactinib Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Defactinib manufacturers

Career Henan Chemical Co

Product: Defactinib 1073154-85-4
Price: US $1.00/KG
Min. Order: 1KG
Purity: 97%
Supply Ability: 200kg
Release date: 2020-02-01

1073154-85-4, DefactinibRelated Search:

Geldanamycin 17-AAG Vorinostat Sunitinib Malate PF 04554878 hydrochloride ODM-201 Y27632 (hydrochloride) ABT-199 SR2516 Trametinib Galeterone Olaparib

Defactinib

VS 6063

VS6063

VS-6063

Defactinib(PF-04554878)

N-methyl-4-(4-((3-(N-methylmethan-3-ylsulfonamido)pyrazin-2-yl)methylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)benzamide

N-Methyl-4-[[4-[[[3-[methyl(methylsulfonyl)amino]-2-pyrazinyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]benzamide

N-METHYL-4-(4-((3-(N-METHYLMETHYL SULFON

N-methyl-4-[[4-[[3-[methyl(methylsulfonyl)amino]pyrazin-2-yl]methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]amino]benzamide

Defactinib (VS-6063

N-methyl-4-(4-((3-(N-methylmethylsulfonamido)pyrazin-2-yl)methylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)benzamide

VS-6063; PF-04554878

PF-04554878 Defactinib

N-methyl-4-((4-(((3-(N-methylmethylsulfonamido)pyrazin-2-yl)methyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)benzamide Defactinib(PF-04554878)(VS-6063)

VS-6063; VS6063; VS 6063; PF04554878; PF-04554878; PF 04554878

CS-1796

Benzamide, N-methyl-4-[[4-[[[3-[methyl(methylsulfonyl)amino]-2-pyrazinyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-

Defactinib free base

Defactinib, FAK inhibitor

Defactinib, 10 mM in DMSO

PF-941222

1073154-85-4

C20H21F3N8O3S

Inhibitors

API