Cat. No.: HY-13007

PF-3758309

(Synonyms: PF-03758309)

11 Cited Publications

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Based on 11 publication(s) in Google Scholar

PF-3758309 (PF-03758309) is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (K_d= 2.7 nM; K_i=18.7 nM). PF-3758309 has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.

For research use only. We do not sell to patients.

Purity: 99.79%
CAS No.: 898044-15-0
Formula: C₂₅H₃₀N₈OS
Molecular Weight:490.62

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

PF-3758309 Chemical Structure

CAS No.: 898044-15-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (11)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
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Biological Activity

Description

IC₅₀ & Target^[1]

PAK4

18.7 nM (Ki)

PAK1

13.7 nM (Ki)

PAK5

18.1 nM (Ki)

PAK6

17.1 nM (Ki)

PAK2

190 nM (IC₅₀)

PAK3

99 nM (IC₅₀)

PAK4

2.7 nM (Kd)

All PAK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.463 μM Compound: PF-3758309	Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay	[PMID: 29886323]
A549	IC₅₀	0.67 μM Compound: 1; PF-3758309	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 24 hrs by CCK8 assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 24 hrs by CCK8 assay	[PMID: 37864885]
A549	IC₅₀	20 nM Compound: 1; PF-3758309	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 3 days by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 3 days by CellTiter-Glo luminescent cell viability assay	[PMID: 37864885]
A549	IC₅₀	20 nM Compound: PF-3758309	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
A549	IC₅₀	27.38 nM Compound: PF-3758309	Inhibition of anchorage independent cell growth in human A549 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis Inhibition of anchorage independent cell growth in human A549 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis	[PMID: 20439741]
ASPC1	IC₅₀	1800 nM Compound: PF-3758309	Antiproliferative activity against human ASPC1 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human ASPC1 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
BT-20	IC₅₀	81.7 nM Compound: PF-3758309	Antiproliferative activity against human BT-20 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human BT-20 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
BT-474	IC₅₀	1.8 nM Compound: PF-3758309	Antiproliferative activity against human BT-474 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human BT-474 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
BT-549	IC₅₀	0.41 nM Compound: PF-3758309	Antiproliferative activity against human BT-549 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human BT-549 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
BXPC-3	IC₅₀	39 nM Compound: PF-3758309	Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
Caco-2	IC₅₀	10000 nM Compound: PF-3758309	Antiproliferative activity against human Caco-2 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human Caco-2 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
Calu-1	IC₅₀	167 nM Compound: PF-3758309	Antiproliferative activity against human Calu-1 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human Calu-1 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
Calu-6	IC₅₀	7.3 nM Compound: PF-3758309	Antiproliferative activity against human Calu-6 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human Calu-6 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
CAMA-1	IC₅₀	2.7 nM Compound: PF-3758309	Antiproliferative activity against human CAMA-1 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human CAMA-1 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
CAPAN-1	IC₅₀	1099 nM Compound: PF-3758309	Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
Capan-2	IC₅₀	136 nM Compound: PF-3758309	Antiproliferative activity against human Capan-2 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human Capan-2 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
CFPAC-1	IC₅₀	1320 nM Compound: PF-3758309	Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
COLO 205	IC₅₀	140.2 nM Compound: PF-3758309	Inhibition of anchorage independent cell growth in human COLO 205 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis Inhibition of anchorage independent cell growth in human COLO 205 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis	[PMID: 20439741]
COLO 205	IC₅₀	2.8 nM Compound: PF-3758309	Antiproliferative activity against human COLO 205 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human COLO 205 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
COLO 320DM	IC₅₀	205 nM Compound: PF-3758309	Antiproliferative activity against human COLO 320DM cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human COLO 320DM cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
COLO 320DM	IC₅₀	373.4 nM Compound: PF-3758309	Inhibition of anchorage independent cell growth in human COLO 320DM cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis Inhibition of anchorage independent cell growth in human COLO 320DM cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis	[PMID: 20439741]
DAN-G	IC₅₀	518 nM Compound: PF-3758309	Antiproliferative activity against human DAN-G cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human DAN-G cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
DLD-1	IC₅₀	10000 nM Compound: PF-3758309	Antiproliferative activity against human DLD-1 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human DLD-1 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
HCC1187	IC₅₀	0.24 nM Compound: PF-3758309	Antiproliferative activity against human HCC1187 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human HCC1187 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
HCC1395	IC₅₀	1.6 nM Compound: PF-3758309	Antiproliferative activity against human HCC1395 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human HCC1395 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
HCC1419	IC₅₀	0.79 nM Compound: PF-3758309	Antiproliferative activity against human HCC1419 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human HCC1419 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
HCC1806	IC₅₀	1.2 nM Compound: PF-3758309	Antiproliferative activity against human HCC1806 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human HCC1806 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
HCC1954	IC₅₀	0.33 nM Compound: PF-3758309	Antiproliferative activity against human HCC1954 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human HCC1954 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
HCC38	IC₅₀	0.52 nM Compound: PF-3758309	Antiproliferative activity against human HCC38 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human HCC38 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
HCC4006	IC₅₀	3.79 nM Compound: PF-3758309	Inhibition of anchorage independent cell growth in human HCC4006 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis Inhibition of anchorage independent cell growth in human HCC4006 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis	[PMID: 20439741]
HCC70	IC₅₀	0.23 nM Compound: PF-3758309	Antiproliferative activity against human HCC70 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human HCC70 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
HCC827	IC₅₀	2.18 nM Compound: PF-3758309	Inhibition of anchorage independent cell growth in human HCC827 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis Inhibition of anchorage independent cell growth in human HCC827 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis	[PMID: 20439741]
HCC827	IC₅₀	9.2 nM Compound: PF-3758309	Antiproliferative activity against human HCC827 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human HCC827 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
HCT-116	IC₅₀	0.039 μM Compound: PF-3758309	Antiproliferative activity against human HCT116 cells after 72 hrs by CCK8 assay Antiproliferative activity against human HCT116 cells after 72 hrs by CCK8 assay	[PMID: 29886323]
HCT-116	IC₅₀	0.24 nM Compound: PF-3758309	Inhibition of anchorage independent cell growth in human HCT-116 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis Inhibition of anchorage independent cell growth in human HCT-116 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis	[PMID: 20439741]
HCT-116	IC₅₀	2.4 nM Compound: PF-3758309	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
HCT-15	IC₅₀	10000 nM Compound: PF-3758309	Antiproliferative activity against human HCT-15 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human HCT-15 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
HEK-293T	IC₅₀	>10 μM Compound: 1; PF-3758309	Antiproliferative activity against HEK293T cells assessed as inhibition of cell growth incubated for 24 hrs by CCK8 assay Antiproliferative activity against HEK293T cells assessed as inhibition of cell growth incubated for 24 hrs by CCK8 assay	[PMID: 37864885]
Hepatocyte	IC₅₀	>1000 nM Compound: PF-3758309	Cytotoxicity against primary hepatocyte (unknown origin) assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Cytotoxicity against primary hepatocyte (unknown origin) assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
HPAC	IC₅₀	265 nM Compound: PF-3758309	Antiproliferative activity against human HPAC cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human HPAC cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
HPAF-II	IC₅₀	517 nM Compound: PF-3758309	Antiproliferative activity against human HPAF-II cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human HPAF-II cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
Hs 766	IC₅₀	416 nM Compound: PF-3758309	Antiproliferative activity against human Hs766T cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human Hs766T cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
Hs-578T	IC₅₀	0.37 nM Compound: PF-3758309	Antiproliferative activity against human Hs-578T cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human Hs-578T cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
HT-29	IC₅₀	4.3 nM Compound: PF-3758309	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
HuP-T3	IC₅₀	280 nM Compound: PF-3758309	Antiproliferative activity against human HuP-T3 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human HuP-T3 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
HuP-T4	IC₅₀	231 nM Compound: PF-3758309	Antiproliferative activity against human HuP-T4 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human HuP-T4 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
LS-123	IC₅₀	10000 nM Compound: PF-3758309	Antiproliferative activity against human LS-123 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human LS-123 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
LS174T	IC₅₀	7.2 nM Compound: PF-3758309	Antiproliferative activity against human LS174T cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human LS174T cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
MCF10	IC₅₀	0.21 nM Compound: PF-3758309	Antiproliferative activity against human MCF10 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human MCF10 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
MCF7	IC₅₀	44.6 nM Compound: PF-3758309	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
MDA-MB-157	IC₅₀	145 nM Compound: PF-3758309	Antiproliferative activity against human MDA-MB-157 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human MDA-MB-157 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
MDA-MB-361	IC₅₀	6.9 nM Compound: PF-3758309	Antiproliferative activity against human MDA-MB-361 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human MDA-MB-361 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
MDA-MB-415	IC₅₀	36 nM Compound: PF-3758309	Antiproliferative activity against human MDA-MB-415 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human MDA-MB-415 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
MDA-MB-436	IC₅₀	0.79 nM Compound: 1, PF-3758309	Cytotoxicity against human MDA-MB-436 cells assessed as reduction in cell viability after 24 to 48 hrs by Celltiter-glo luminescence assay Cytotoxicity against human MDA-MB-436 cells assessed as reduction in cell viability after 24 to 48 hrs by Celltiter-glo luminescence assay	[PMID: 24432870]
MDA-MB-436	IC₅₀	0.79 nM Compound: PF-3758309	Antiproliferative activity against human MDA-MB-436 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human MDA-MB-436 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
MDA-MB-453	IC₅₀	13.3 nM Compound: PF-3758309	Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
MDA-MB-468	IC₅₀	0.63 nM Compound: PF-3758309	Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
MIA PaCa-2	IC₅₀	17 nM Compound: PF-3758309	Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
NCI-H1299	IC₅₀	7 nM Compound: PF-3758309	Inhibition of anchorage independent cell growth in human NCI-H1299 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis Inhibition of anchorage independent cell growth in human NCI-H1299 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis	[PMID: 20439741]
NCI-H1355	IC₅₀	14.2 nM Compound: PF-3758309	Inhibition of anchorage independent cell growth in human NCI-H1355 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis Inhibition of anchorage independent cell growth in human NCI-H1355 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis	[PMID: 20439741]
NCI-H1395	IC₅₀	6.4 nM Compound: PF-3758309	Antiproliferative activity against human NCI-H1395 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H1395 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
NCI-H1395	IC₅₀	7.62 nM Compound: PF-3758309	Inhibition of anchorage independent cell growth in human NCI-H1395 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis Inhibition of anchorage independent cell growth in human NCI-H1395 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis	[PMID: 20439741]
NCI-H1437	IC₅₀	4.8 nM Compound: PF-3758309	Inhibition of anchorage independent cell growth in human NCI-H1437 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis Inhibition of anchorage independent cell growth in human NCI-H1437 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis	[PMID: 20439741]
NCI-H1573	IC₅₀	2.37 nM Compound: PF-3758309	Inhibition of anchorage independent cell growth in human NCI-H1573 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis Inhibition of anchorage independent cell growth in human NCI-H1573 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis	[PMID: 20439741]
NCI-H1573	IC₅₀	22 nM Compound: PF-3758309	Antiproliferative activity against human NCI-H1573 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H1573 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
NCI-H1581	IC₅₀	0.6 nM Compound: PF-3758309	Antiproliferative activity against human NCI-H1581 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H1581 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
NCI-H1650	IC₅₀	5.57 nM Compound: PF-3758309	Inhibition of anchorage independent cell growth in human NCI-H1650 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis Inhibition of anchorage independent cell growth in human NCI-H1650 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis	[PMID: 20439741]
NCI-H1651	IC₅₀	20 nM Compound: PF-3758309	Antiproliferative activity against human NCI-H1651 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H1651 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
NCI-H1666	IC₅₀	3.8 nM Compound: PF-3758309	Antiproliferative activity against human NCI-H1666 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H1666 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
NCI-H1666	IC₅₀	6.25 nM Compound: PF-3758309	Inhibition of anchorage independent cell growth in human NCI-H1666 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis Inhibition of anchorage independent cell growth in human NCI-H1666 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis	[PMID: 20439741]
NCI-H1703	IC₅₀	4.4 nM Compound: PF-3758309	Antiproliferative activity against human NCI-H1703 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H1703 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
NCI-H1734	IC₅₀	4.1 nM Compound: PF-3758309	Antiproliferative activity against human NCI-H1734 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H1734 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
NCI-H1755	IC₅₀	15 nM Compound: PF-3758309	Antiproliferative activity against human NCI-H1755 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H1755 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
NCI-H1770	IC₅₀	1.84 nM Compound: PF-3758309	Inhibition of anchorage independent cell growth in human NCI-H1770 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis Inhibition of anchorage independent cell growth in human NCI-H1770 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis	[PMID: 20439741]
NCI-H1838	IC₅₀	5.5 nM Compound: PF-3758309	Antiproliferative activity against human NCI-H1838 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H1838 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
NCI-H1838	IC₅₀	9.59 nM Compound: PF-3758309	Inhibition of anchorage independent cell growth in human NCI-H1838 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis Inhibition of anchorage independent cell growth in human NCI-H1838 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis	[PMID: 20439741]
NCI-H1975	IC₅₀	17 nM Compound: PF-3758309	Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
NCI-H1993	IC₅₀	11.95 nM Compound: PF-3758309	Inhibition of anchorage independent cell growth in human NCI-H1993 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis Inhibition of anchorage independent cell growth in human NCI-H1993 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis	[PMID: 20439741]
NCI-H2087	IC₅₀	1.36 nM Compound: PF-3758309	Inhibition of anchorage independent cell growth in human NCI-H2087 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis Inhibition of anchorage independent cell growth in human NCI-H2087 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis	[PMID: 20439741]
NCI-H2087	IC₅₀	4.3 nM Compound: PF-3758309	Antiproliferative activity against human NCI-H2087 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H2087 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
NCI-H2170	IC₅₀	6.04 nM Compound: PF-3758309	Inhibition of anchorage independent cell growth in human NCI-H2170 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis Inhibition of anchorage independent cell growth in human NCI-H2170 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis	[PMID: 20439741]
NCI-H226	IC₅₀	9.3 nM Compound: PF-3758309	Antiproliferative activity against human NCI-H226 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H226 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
NCI-H23	IC₅₀	25 nM Compound: PF-3758309	Antiproliferative activity against human NCI-H23 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H23 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
NCI-H23	IC₅₀	3.45 nM Compound: PF-3758309	Inhibition of anchorage independent cell growth in human NCI-H23 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis Inhibition of anchorage independent cell growth in human NCI-H23 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis	[PMID: 20439741]
NCI-H2347	IC₅₀	2 nM Compound: PF-3758309	Antiproliferative activity against human NCI-H2347 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H2347 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
NCI-H358	IC₅₀	11 nM Compound: PF-3758309	Antiproliferative activity against human NCI-H358 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H358 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
NCI-H358	IC₅₀	7.7 nM Compound: PF-3758309	Inhibition of anchorage independent cell growth in human NCI-H358 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis Inhibition of anchorage independent cell growth in human NCI-H358 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis	[PMID: 20439741]
NCI-H441	IC₅₀	9.2 nM Compound: PF-3758309	Antiproliferative activity against human NCI-H441 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H441 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
NCI-H520	IC₅₀	1.13 nM Compound: PF-3758309	Inhibition of anchorage independent cell growth in human NCI-H520 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis Inhibition of anchorage independent cell growth in human NCI-H520 cells incubated for 6 days by Alamar blue reagent based fluorescence plate reader analysis	[PMID: 20439741]
NCI-H520	IC₅₀	5.6 nM Compound: PF-3758309	Antiproliferative activity against human NCI-H520 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H520 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
NCI-H526	IC₅₀	1.4 nM Compound: PF-3758309	Antiproliferative activity against human NCI-H526 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H526 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
NCI-H647	IC₅₀	36 nM Compound: PF-3758309	Antiproliferative activity against human NCI-H647 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H647 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
NCI-H716	IC₅₀	11 nM Compound: PF-3758309	Antiproliferative activity against human NCI-H716 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H716 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
NCI-H82	IC₅₀	2.1 nM Compound: PF-3758309	Antiproliferative activity against human NCI-H82 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H82 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
PANC-03-27	IC₅₀	32 nM Compound: PF-3758309	Antiproliferative activity against human PANC-03-27 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human PANC-03-27 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
PANC-08-13	IC₅₀	12 nM Compound: PF-3758309	Antiproliferative activity against human PANC-08-13 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human PANC-08-13 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
PANC-1	IC₅₀	856 nM Compound: PF-3758309	Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
Panc1005	IC₅₀	67 nM Compound: PF-3758309	Antiproliferative activity against human Panc1005 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human Panc1005 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
PaTu 8988t	IC₅₀	73 nM Compound: PF-3758309	Antiproliferative activity against human PaTu 8988t cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent cell viability assay Antiproliferative activity against human PaTu 8988t cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent cell viability assay	[PMID: 20439741]
PSN1	IC₅₀	34 nM Compound: PF-3758309	Antiproliferative activity against human PSN1 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human PSN1 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
RKO	IC₅₀	1.8 nM Compound: PF-3758309	Antiproliferative activity against human RKO cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human RKO cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
SK-BR-3	IC₅₀	132 nM Compound: PF-3758309	Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
SK-MES-1	IC₅₀	3.2 nM Compound: PF-3758309	Antiproliferative activity against human SK-MES-1 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-MES-1 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
SU.86.86	IC₅₀	898 nM Compound: PF-3758309	Antiproliferative activity against human SU-86-86 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SU-86-86 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
SW1990	IC₅₀	127 nM Compound: PF-3758309	Antiproliferative activity against human SW1990 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SW1990 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
SW-620	IC₅₀	5.7 nM Compound: PF-3758309	Antiproliferative activity against human SW620 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SW620 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
SW948	IC₅₀	4.3 nM Compound: PF-3758309	Antiproliferative activity against human SW948 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SW948 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
T47D	IC₅₀	0.99 nM Compound: PF-3758309	Antiproliferative activity against human T47D cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human T47D cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
T84	IC₅₀	89 nM Compound: PF-3758309	Antiproliferative activity against human T84 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human T84 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]
ZR-75-1	IC₅₀	0.49 nM Compound: PF-3758309	Antiproliferative activity against human ZR-75-1 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human ZR-75-1 cells assessed as inhibition of cell proliferation incubated for 3 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 20439741]

In Vitro

PF-3758309 has similar enzymatic potency against the kinase domains of the other group B PAKs (PAK5, K_i=18.1 nM; PAK6, K_i=17.1 nM) and group A PAK1 (K_i=13.7 nM), but is less active against the other two group A PAKs (PAK2, IC₅₀=190 nM; PAK3, IC₅₀=99 nM)^[1].
In cells, PF-3758309 inhibits phosphorylation of the PAK4 substrate GEF-H1 (IC₅₀=1.3 nM) and anchorage-independent growth of a panel of tumor cell lines (IC₅₀=4.7 nM)^[1].
PF-3758309 also inhibits endogenous pGEF-H1 accumulation in HCT116 cells. PF-3758309 potently inhibits cellular proliferation (IC₅₀=20 nM) and anchorage-independent growth (IC₅₀=27 nM) of A549 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PF-3758309 (7.5-30 mg/kg; p.o.; twice daily for 9-18 days) results in statistically significant tumor growth inhibition (TGI) in HCT116 and A549 models^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female nu/nu, CRL breed 6–8 weeks old mice (bearing HCT116 and A549 tumors)^[1]
Dosage:

7.5-30 mg/kg
Administration:

Oral administration; twice daily for 9-18 days
Result:

Significant tumor growth inhibition (TGI) in HCT116 and A549 models.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 898044-15-0
Appearance Solid
Molecular Weight 490.62
Formula C₂₅H₃₀N₈OS
Color White to light yellow
SMILES

CC1=NC2=C(SC=C2)C(NC3=NNC4=C3CN(C(N[C@@H](C5=CC=CC=C5)CN(C)C)=O)C4(C)C)=N1
Synonyms

PF-03758309
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (11)

All

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Journal Impact Factor

Science

The target landscape of clinical kinase drugs. [Abstract]

2017 Dec 1;358(6367):eaan4368. PMID: 29191878
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Int J Mol Sci

Inhibition of NAMPT by PAK4 Inhibitors. [Abstract]

2024 Sep 21;25(18):10138. PMID: 39337621
Biochem J

Up-regulation of the PI3K/AKT and RHO/RAC/PAK signalling pathways in CHK1 inhibitor resistant Eµ-Myc lymphoma cells. [Abstract]

2022 Oct 14;479(19):2131-2151. PMID: 36240067
Exp Cell Res

PAK5 promotes the cell stemness ability by phosphorylating SOX2 in lung squamous cell carcinomas. [Abstract]

2020 Oct 15;395(2):112187. PMID: 32721391
Anticancer Drugs

AZD7762 induces CRBN dependent BAG3 degradation through ubiquitin-proteasome pathway. [Abstract]

2024 Jan 1;35(1):46-54. PMID: 37449977
bioRxiv

2026 May 29.
bioRxiv

2025 April 26.
bioRxiv

Network analysis of α-synuclein pathology progression reveals p21-activated kinases as regulators of vulnerability. [Abstract]

2024 Oct 22:2024.10.22.619411. PMID: 39484617
Necmettin Erbakan University

2022 Jun.

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (203.82 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0382 mL

10.1912 mL

20.3824 mL

5 mM

0.4076 mL

2.0382 mL

4.0765 mL

10 mM

0.2038 mL

1.0191 mL

2.0382 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.10 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.10 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.10 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Murray, Brion W., et al. Small-molecule p21-activated kinase inhibitor PF3758309 is a potent inhibitor of oncogenic signaling and tumor growth. Proceedings of the National Academy of Sciences of the United States of America (2010), 107(20), 9446-9451, S94 [Content Brief]

[2]. Zhao ZS, et al. Do PAKs make good drug targets? F1000 Biol Rep. 2010 Sep 23;2:70. [Content Brief]

[3]. Ryu BJ, et al. PF-3758309, p21-activated kinase 4 inhibitor, suppresses migration and invasion of A549 human lung cancer cells via regulation of CREB, NF-κB, and β-catenin signalings. Mol Cell Biochem. 2014 Apr;389(1-2):69-77. [Content Brief]

[4]. Pitts TM, et al. Association of the epithelial-to-mesenchymal transition phenotype with responsiveness to the p21-activated kinase inhibitor, PF-3758309, in colon cancer models. Front Pharmacol. 2013 Mar 28;4:35. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0382 mL	10.1912 mL	20.3824 mL	50.9559 mL
	5 mM	0.4076 mL	2.0382 mL	4.0765 mL	10.1912 mL
	10 mM	0.2038 mL	1.0191 mL	2.0382 mL	5.0956 mL
	15 mM	0.1359 mL	0.6794 mL	1.3588 mL	3.3971 mL
	20 mM	0.1019 mL	0.5096 mL	1.0191 mL	2.5478 mL
	25 mM	0.0815 mL	0.4076 mL	0.8153 mL	2.0382 mL
	30 mM	0.0679 mL	0.3397 mL	0.6794 mL	1.6985 mL
	40 mM	0.0510 mL	0.2548 mL	0.5096 mL	1.2739 mL
	50 mM	0.0408 mL	0.2038 mL	0.4076 mL	1.0191 mL
	60 mM	0.0340 mL	0.1699 mL	0.3397 mL	0.8493 mL
	80 mM	0.0255 mL	0.1274 mL	0.2548 mL	0.6369 mL
	100 mM	0.0204 mL	0.1019 mL	0.2038 mL	0.5096 mL

Keywords

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

PF-3758309

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Chemical Probe Library

Targeted Diversity Library

Heterocyclic Compound Library

Cell Death Library

Multi-Target Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) PF-3758309

All PAK Isoforms

Biological Activity

Chemical Information

Publications (11)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PF-3758309

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Chemical Probe Library

Targeted Diversity Library

Heterocyclic Compound Library

Cell Death Library

Multi-Target Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) PF-3758309

All PAK Isoforms

Biological Activity

Chemical Information

Publications (11)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PF-3758309 Related Classifications

Cat. No.: HY-13007