PD 0332991 HCl Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

PD 0332991 is an orally active, selective inhibitor of the cyclin D kinases Cdk4 (IC₅₀ = 11 nM) and Cdk6 (IC₅₀= 16 nM) with no activity against a panel of 36 additional protein kinases. It has been reported to have antiproliferative activity against retinoblastoma-positive tumor cells, blocking retinoblastoma phosphorylation and inducing G₁ arrest at nanomolar concentrations. PD 0332991 can inhibit the growth of certain ER-positive or HER2-amplified breast cancer cells (IC₅₀s as low as 4 nM) and demonstrates synergy with tamoxifen and trastuzumab, respectively. PD 0332991 inhibition of Cdk4 activity has been used to demonstrate a role for insulin-activated cyclinD1-Cdk4 signaling in the control of glucose metabolism that is independent of cell cycle progression.

Allgemeine Beschreibung

A cell-permeable, orally available and brain permeant, non-toxic pyridopyrimidinone compound that acts as a potent, selective, reversible, ATP competitive inhibitor of Cdk4 and Cdk6 (IC₅₀ = 11, 9, and 15 nM for Cdk4/D1, Cdk4/D3 and Cdk6/D2, respectively). Hence, it reduces retinoblastoma protein phosphorylation at Ser780/Ser795 (IC₅₀ = 66 nM in MDA-435 cells) and arrests cell cycle at G1 phase. Acts as a cytostatic agent, but does induce apoptotic cell death when used alone. However, it potentiates the cytotoxicity of dexamethasone (>Cat. No. 265005), bortezomib (>Cat. No. 504314), and tamoxifen (Cat. No. 579000) in estrogen receptor (ER)-positive cell lines. Exhibits only a trivial inhibitory activity towards Cdk2/E2, Cdk2/A, Cdk1/B and Cdk5/p25 in a 36-kinase panel (IC₅₀ >10 μM). Improves endoderm differentiation of late G1-human embryonic stem cells expressing Smad2 or Smad3 (~ 750 nM) and further enhances endoderm differentiation into hepatic and pancreatic progenitor cells. Shown to regress the growth of human breast tumor xenografts in murine models (~150 mg/kg, p.o., daily).

Biochem/physiol Actions

Cell permeable: yes

PD 0332991 HCl Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

PD 0332991 HCl Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
Henan Fengda Chemical Co., Ltd	+86-371-86557731 +86-13613820652	info@fdachem.com	China	20122	58
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21587	55
Nanjing Finetech Chemical Co., Ltd.	025-85710122 17714198479	sales@fine-chemtech.com	CHINA	885	55
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	33024	60
career henan chemical co	+86-0371-86658258 +8613203830695	sales@coreychem.com	China	29815	58
Biochempartner	0086-13720134139	candy@biochempartner.com	CHINA	965	58
Jinan Shengqi pharmaceutical Co,Ltd	86+18663751872	christine@shengqipharm.com	CHINA	491	58
BOC Sciences	+1-631-485-4226	inquiry@bocsci.com	United States	19936	58
ANHUI WITOP BIOTECH CO., LTD	+8615255079626	eric@witopchemical.com	China	23541	58
Dideu Industries Group Limited	+86-29-89586680 +86-15129568250	1026@dideu.com	China	20582	58

827022-32-2()Verwandte Suche:

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• PD 0332991 HCl
• PALBOCICLIB HCL; PD0332991 HCL
• 6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride Palbociclib (PD-0332991) HCl
• Palbociclib hydrochloride, >=98%
• PD-0332991 (Palbociclib)
• PD 0332991 hydrochloride
• Palbociclib (hydrochloride)
• Palbociclib (PD-0332991) HCl
• 6-acetyl-8-cyclopentyl-5-Methyl-2-(5-(piperazin-1-yl)pyridin-2-ylaMino)pyrido[2,3-d]pyriMidin-7(8H)-one hydrochloride
• Pyrido[2,3-d]pyrimidin-7(8H)-one,6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]-,monohydrochloride
• Palbociclib (PD-0332991) hydrochloride
• 6-acetyl-8-cyclopentyl-5-methyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one hydrochloride
• 6-Acetyl-8-cyclopentyl-5-methyl-2-(5-(piperazin-1-yl)pyridin-2-ylamino)pyrido[2,3-d]pyrimidin-
• 6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one Hydrochloride
• PD 0332991 HCl (Palbociclib)
• Palbociclib-025
• PD 0332991 (Palbociclib) HCl
• CS-365
• Palbociclib-019-HCl
• PD 0332991;PD-0332991
• Palbociclib hydrochloride, 99%, a highly selective CDK4/6 inhibitor
• PALBOCICLIB;PD-0332991 HYDROCHLORIDE;PD0332991 HYDROCHLORIDE;PD 0332991 HYDROCHLORIDE
• Palbociclib, brand name: Ibrance
• PD 0332991; PD-0332991; PD0332991; PD0332991; PD332991; PD-332991; PD 332991; PALBOCICLIB, BRAND NAME: IBRANCE
• PD 0332991 HCl USP/EP/BP
• Pyrido[2,3-d]pyrimidin-7(8H)-one,6-acetyl-8-cyclopentyl-5-me...
• Palbociclib (monohydrochloride)
• TIANFU-CHEM CAS:827022-32-2 PD 0332991 HCl
• 6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride1
• PALBOCICLIB (PD-0332991) (HCL SALT)
• Palbociclib Impurity 22 HCl
• Palbociclib Impurity 20 HCl
• PD 0332991 hydrochloride(1:1)
• StemSelect PD 0332991
• PD-0332991 HCl (Palbociclib HCl)
• 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 (PD-0332991 hydrochloride
• 6-ethylacyl-8-cyclopentyl-5-methyl-2-[[5-(azine-1-yl)pyridine-2-yl]amino]-8H-pyridinebenzo[2,3-d]pyrimidine-7-onehydrochloride
• Palbociclib HCl
• 827022-32-2
• C24H29N7O2HCl
• C24H30ClN7O2
• C24H29N7O2ClH
• Inhibitors