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1073154-85-4 (Defactinib)

1

Identification

Defactinib Defactinib
Name Defactinib
Formula C20H21F3N8O3S
MW 510.49
CAS No. 1073154-85-4
EINECS
Smiles O=C(NC)C1=CC=C(NC2=NC=C(C(F)(F)F)C(NCC3=NC=CN=C3N(C)S(=O)(C)=O)=N2)C=C1
Synonyms VS-6063;VS6063;VS 6063; N-methyl-4-((4-(((3-(N-methylmethylsulfonamido)pyrazin-2-yl)methyl)amino)-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)
2

Introduction

Defactinib is a novel FAK inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.

Background Information

A non-receptor tyrosine kinase ......by AOBIOUS INC
The combination of VS-6063 and paclitaxel synergistically decreases proliferation and increases apoptosis in SKOV3ip1, SKOV3-TR, HeyA8 and HeyA8-MDR cells. In both PTX-sensitive and PTX-resistant models, VS-6063 (50 mg/kg p.o.) enhances tumor growth inhibition by paclitaxel. ......by AbMole BioScience
PF-04554878 is a novel FAK kinase inhibitor that decreases growth and induces apoptosis in pancreatic neuroendocrine tumor cells ......by AdooQ BioScience, LLC
Defactinib, also known as VS-6063 and PF-04554878, is an orally bioavailable, small-molecule focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. FAK inhibitor PF-04554878 inhibits FAK, which may prevent the ......by BOC Sciences
PF-04554878 is potent, ATP-competitive, focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. PF-04554878 inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner. A combination of PF-04554878 and paclitaxel markedly decreases proliferation and increases apoptosis. ......by BioVision, Inc.,
Defactinib is a novel FAK inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner. ......by MedChemexpress Co., Ltd.
Defactinib, also known as VS-6063 and PF-04554878, is an orally bioavailable, small-molecule focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. FAK inhibitor PF-04554878 inhibits FAK, which may prevent the integrin-mediated activation of several downstream signal transduction pathways, including ERK, JNK/MAPK and PI3K/Akt, thus inhibiting tumor cell migration, proliferation and survival. ......by MedKoo Biosciences, Inc.
Defactinib (VS-6063, PF-04554878) is a potent, selective and orally active FAK inhibitor, selectively inhibits pFAK (Tyr397) in a dose-dependent manner in cancer cell lines; shows no statistically significant changes in FAK phosphorylation at the other residues(Tyr 576/577, Tyr 925, or Tyr 861), also inhibits Pyk2 Tyr402 phosphorylation in HeyA8 cells; markedly decreases proliferation and increases apoptosis combined with paclitaxel, reduces levels of AKT and YB-1 in taxane-resistant cell lines; significantly reduces tumor growth, synergized with the mTOR inhibitor everolimus in xenograft models of pancreatic tumor.Lung CancerPhase 2 Clinical ......by ProbeChem
Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2. ......by Selleck Chemicals LLC
Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2. ......by Target Molecule Corp.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000010035

Storage condition

4°C by MedChemexpress Co., Ltd.

Solubility

DMSO 50 mg/ml by CHEMSCENE, LLC
DMSO 50 mg/ml by MedChemexpress Co., Ltd.
5

Mechanism and Indication

Signaling Pathways Protein Tyrosine Kinase/RTK
Target FAK
Research Area Cancer
Indications Non Hematologic Cancers
6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Defactinib Verastem, Inc. Non Hematologic Cancers 2013/9/11 Phase 1 Clinical
Defactinib - Phase 2
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Safety Data of Defactinib

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
AOBIOUS INC 1mg/USD17() USA
AbMole BioScience USA
Active Biochem 10mg/USD110() USA
AdooQ BioScience, LLC 5mg/USD320() USA
Apexbio Technology LLC 5mg/USD105(In stock) USA
Ark Pharm, Inc. USA
BOC Sciences
BioVision, Inc., 5mg/USD175() USA
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD84();10mg/USD108() USA
Cayman Chemical Company 1mg/USD29() USA
ChemieTek 10mg/USD120();200mg/USD700() USA
DC Chemicals 100mg/USD400(In stock) China
MedChemexpress Co., Ltd. 5mg/USD84();10mg/USD108() USA
MedKoo Biosciences, Inc. 10mg/USD120() USA
ProbeChem
Selleck Chemicals LLC USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD84();10mg/USD108() China
Target Molecule Corp. 5mg/USD101();10mg/USD198();25mg/USD356();50mg/USD546();100mg/USD899() USA
10

Related Products

Other Forms of 1073154-85-4

Name CAS No Formula MW
Defactinib (hydrochloride) 1073160-26-5 C20H22ClF3N8O3S 546.95

Recommended Compounds in FAK

Name CAS No Formula MW
CEP-37440 1391712-60-9 C30H38ClN7O3 580.12
PND-1186 1061353-68-1 C25H26F3N5O3 501.5
PF-573228 869288-64-2 C22H20F3N5O3S 491.4861
PF-562271 (besylate) 939791-38-5 C27H26F3N7O6S2 665.66
NVP-TAE 226 761437-28-9 C23H25ClN6O3 468.94
PF-431396 717906-29-1 C22H21F3N6O3S 506.5
PF-562271 717907-75-0 C21H20F3N7O3S 507.49
Y15 4506-66-5 C6H14Cl4N4 284.0142
NAMI-A 201653-76-1 C8H16Cl4N4ORuS 459.19
Defactinib (hydrochloride) 1073160-26-5 C20H22ClF3N8O3S 546.95
GSK2256098 1224887-10-8 C20H23ClN6O2 414.8886

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

12

References

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More Information

Defactinib

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