PF-3758309 hydrochloride

Modify Date: 2024-01-09 13:08:57

PF-3758309 hydrochloride structure	Common Name	PF-3758309 hydrochloride
	CAS Number	1279034-84-2	Molecular Weight	483.994
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₅H₃₁ClN₈OS	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of PF-3758309 hydrochloride

PF-3758309 hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation[1][2][3].

Name	Palbociclib HCl
Synonym	More Synonyms

Description	PF-3758309 hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation[1][2][3].
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> Cytoskeleton >> PAK Signaling Pathways >> Cell Cycle/DNA Damage >> PAK
Target	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)
In Vitro	PF-3758309 hydrochloride has similar enzymatic potency against the kinase domains of the other group B PAKs (PAK5, Ki=18.1 nM; PAK6, Ki=17.1 nM) and group A PAK1 (Ki=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 hydrochloride 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 hydrochloride 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].
In Vivo	PF-3758309 hydrochloride (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]. 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.
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. [2]. Zhao ZS, et al. Do PAKs make good drug targets? F1000 Biol Rep. 2010 Sep 23;2:70. [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.

Molecular Formula	C₂₅H₃₁ClN₈OS
Molecular Weight	483.994
Exact Mass	483.214966

Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]-, hydrochloride (1:1)

Palbociclib hydrochloride

UNII:BKC4F3Q5XL

Palbociclib HCl

6-Acetyl-8-cyclopentyl-5-methyl-2-{[5-(1-piperazinyl)-2-pyridinyl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride (1:1)

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: PF-03758309 (hydrochloride)
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

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