• Search chemicals, activators, Inhibitors, APIs, intermediates and raw materials.

1061353-68-1 (PND-1186)

1

Identification

PND-1186 PND-1186
Name PND-1186
Formula C25H26F3N5O3
MW 501.5
CAS No. 1061353-68-1
EINECS
Smiles O=C(NC)C1=CC=CC=C1NC2=CC(NC3=CC=C(N4CCOCC4)C=C3OC)=NC=C2C(F)(F)F
Synonyms SR-2516;PND 1186;PND1186;SR 2516;SR2516; 2-((2-((2-methoxy-4-morpholinophenyl)amino)-5-(trifluoromethyl)pyridin-4-yl)amino)-N-methylbenzamide
InChI InChI=1S/C25H26F3N5O3/c1-29-24(34)17-5-3-4-6-19(17)31-21-14-23(30-15-18(21)25(26,27)28)32-20-8-7-16(13-22(20)35-2)33-9-11-36-12-10-33/h3-8,13-15H,9-12H2,1-2H3,(H,29,34)(H2,30,31,32)
2

Introduction

PND-1186 is a potent FAK inhibitor with IC50 of 1.5 nM. IC50 Value: 1.5 nM [1] Target: FAK in vitro: PND-1186 has an IC50 of ~100 nM in breast carcinoma cells as determined by anti-phospho-specific immunoblotting to FAK Tyr-397.

Background Information

In mice bearing 4T1 tumors, PND-1186 (100 mg/kg s.c.) inhibits 4T1 subcutaneous tumor growth by induction of apoptosis. In mice bearing ID8 tumors, PND-1186 (0.5 mg/mL for p.o.) also causes ovarian carcinoma tumor growth inhibition.Addition of PND-1186 to the drinking water of mice was well tolerated and inhibited ascites- and peritoneal membrane-associated ovarian carcinoma tumor growth associated with the inhibition of FAK Tyr-397 phosphorylation. ......by AbMole BioScience
PND-1186 is a potent FAK inhibitor with IC50 of 1.5 nM. ......by AdooQ BioScience, LLC
Description ......by Apexbio Technology LLC
PND-1186 (VS-4718) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. Phase 1. ......by BOC Sciences
PND-1186 is a potent FAK (Focal adhesion kinase) inhibitor (IC₅₀ = 1.5 nM) with potential antineoplastic activity. PND-1186 inhibits FAK, blocks fibronectin-stimulated FAK autophosphorylation of Tyr397, and may prevent the integrin-mediated activation of several downstream signal transduction pathways, including ERK, JNK/MAPK and PI3K/Akt. This results in the reduction of the number of cancer stem cells (CSCs) and inhibits tumor cell migration, proliferation and survival. ......by BioVision, Inc.,
PND-1186 is a substituted pyridine reversible inhibitor of FAK activity with IC50 of 1.5 nM in vitro. ......by MedChemexpress Co., Ltd.
PND-1186, also known as SR-2156 and VS-4718, is a potent FAK inhibitor with a 50% inhibitory concentration (IC50) of 1.5 nM in vitro. PND-1186 has an IC50 of ~100 nM in breast carcinoma cells. Notably, 1.0 µM PND-1186 (>5-fold above IC50) had limited effects on cell proliferation. However, under non-adherent conditions as spheroids and as colonies in soft agar, 0.1 µM PND-1186 blocked FAK and p130Cas tyrosine phosphorylation, promoted caspase-3 activation, and triggered cell apoptosis. PND-1186 inhibited 4T1 breast carcinoma subcutaneous tumor growth correlated with elevated tumor cell apoptosis and caspase 3 activation. ......by MedKoo Biosciences, Inc.
PND-1186 (VS-4718) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. Phase 1. ......by Selleck Chemicals LLC
PND-1186 (VS-4718) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. Phase 1. ......by Target Molecule Corp.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000014015

Storage condition

Solubility

DMSO by MedChemexpress Co., Ltd.
5

Mechanism and Indication

Signaling Pathways Protein Tyrosine Kinase/RTK
Target FAK
Research Area Cancer
Indications Metastasis
6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
PND-1186 Verastem Inc Metastasis 2013/6/30 2014/12/31 Phase 1 Clinical
PND-1186 - Phase 1
7

Safety Data of PND-1186

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AbMole BioScience USA
AdooQ BioScience, LLC USA
Aladdin 5mg/RMB3487() China
Apexbio Technology LLC 5mg/USD110(In stock);100mg/USD550(In stock) USA
Ark Pharm, Inc. USA
BOC Sciences 50mg/USD258(In stock)
BioVision, Inc., 5mg/USD125() USA
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD132();10mg/USD180() USA
Cayman Chemical Company USA
DC Chemicals 100mg/USD480(In stock) China
MedChemexpress Co., Ltd. 5mg/USD132();10mg/USD180() USA
MedKoo Biosciences, Inc. 10mg/USD150() USA
Pure Chemistry Scientific Inc. 5mg/USDnull(In stock) USA
Selleck Chemicals LLC USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD132();10mg/USD180() China
Target Molecule Corp. 2mg/USD85();5mg/USD110();25mg/USD298();100mg/USD396() USA
10

Related Products

Other Forms of 1061353-68-1

Name CAS No Formula MW
PND-1186 (Hydrochloride) 1356154-94-3 C25H27ClF3N5O3 537.96
PND-1186 (TFA salt) 1061353-69-2 C27H27F6N5O5 615.52

Recommended Compounds in FAK

Name CAS No Formula MW
Defactinib 1073154-85-4 C20H21F3N8O3S 510.49
CEP-37440 1391712-60-9 C30H38ClN7O3 580.12
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
AT9283 896466-04-9 C19H23N7O2 381.43
IDO5L 914471-09-3 C9H7ClFN5O2 271.6356
BEZ235 915019-65-7 C30H23N5O 469.54
MK-0752 471905-41-6 C21H21ClF2O4S 442.9
AZD8330 869357-68-6 C16H17FIN3O4 461.23
LY2228820 862507-23-1 C26H37FN6O6S2 612.74
AXL1717 477-47-4 C22H22O8 414.41
Napabucasin 83280-65-3 C14H8O4 240.2109
Icotinib (Hydrochloride) 1204313-51-8 C22H22ClN3O4 427.88
LY2874455 1254473-64-7 C21H19Cl2N5O2 444.31
MI-773 1303607-07-9 C29H34Cl2FN3O3 562.5
AT7519 (trifluoroacetate) 1431697-85-6 C18H18Cl2F3N5O4 496.27
BEZ235 (Tosylate) 1028385-32-1 C37H31N5O4S 641.74
BAY 80-6946 1032568-63-0 C23H28N8O4 480.52
INCB 024360 1204669-58-8 C11H13BrFN7O4S 438.23
LY2801653 1206799-15-6 C30H22F2N6O3 552.53
LY2801653 (dihydrochloride) 1206801-37-7 C30H24Cl2F2N6O3 625.45
LY2835219 (free base) 1231929-97-7 C27H32F2N8 506.59
LY2835219 1231930-82-7 C28H36F2N8O3S 602.7
LY2606368 1234015-52-1 C18H19N7O2 365.39
11

Route of Synthesis

12

References

13

More Information

PND-1186

Tags: buy 1061353-68-1 IC50 | 1061353-68-1 price | 1061353-68-1 cost | 1061353-68-1 solubility | 1061353-68-1 purchase | 1061353-68-1 manufacturer | 1061353-68-1 research buy | 1061353-68-1 order | 1061353-68-1 MSDS | 1061353-68-1 chemical structure | 1061353-68-1 Storage condition | 1061353-68-1 molecular weight | 1061353-68-1 mw | 1061353-68-1 datasheet | 1061353-68-1 supplier | 1061353-68-1 cell line | 1061353-68-1 NMR | 1061353-68-1 MS | 1061353-68-1 IR | 1061353-68-1 solubility | 1061353-68-1 Safe information | 1061353-68-1 Qc and Spectral Information | 1061353-68-1 Clinical Information | 1061353-68-1 Clinical Trial | 1061353-68-1 Route of Synthesis | 1061353-68-1 storage condition | 1061353-68-1 diseases and conditions | 1061353-68-1 flash point | 1061353-68-1 boiling point | 1061353-68-1 melting point | 1061353-68-1 storage condition | 1061353-68-1 brand