Palbociclib hydrochloride | CAS:827022-32-2

Palbociclib hydrochloride

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Description:

Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc.

Targets:

CDK4/6

In vitro:

Cancer Res,2008 Jul 15;68(14):5519-23.

A novel therapeutic combination using PD 0332991 and bortezomib: study in the 5T33MM myeloma model.[Pubmed: 18632601]

Multiple myeloma (MM) remains incurable partly because no effective cell cycle-based therapy has been available to both control tumor cell proliferation and synergize with cytotoxic killing. PD 0332991 is an orally active small molecule that potently and specifically inhibits Cdk4 and Cdk6. It has been shown to induce rapid G(1) cell cycle arrest in primary human myeloma cells and suppress tumor growth in xenograft models.
METHODS AND RESULTS:
To improve therapeutic targeting of myeloma progression, we combined tumor suppression by PD 0332991 with cytotoxic killing by bortezomib, a proteasome inhibitor widely used in myeloma treatment, in the immunocompetent 5T33MM myeloma model. We show that 5T33MM tumor cells proliferate aggressively in vivo due to expression of cyclin D2, elevation of Cdk4, and impaired p27(Kip1) expression, despite inhibition of Cdk4/6 by p18(INK4c) and the maintenance of a normal plasma cell transcription program. PD 0332991 potently inhibits Cdk4/6-specific phosphorylation of Rb and cell cycle progression through G(1) in aggressively proliferating primary 5T33MM cells, in vivo and ex vivo. This leads to tumor suppression and a significant improvement in survival. Moreover, induction of G(1) arrest by PD 0332991 sensitizes 5T33MM tumor cells to killing by bortezomib.
CONCLUSIONS:
Inhibition of Cdk4/6 by PD 0332991, therefore, effectively controls myeloma tumor expansion and sensitizes tumor cells to bortezomib killing in the presence of an intact immune system, thereby representing a novel and promising cell cycle-based combination therapy.

Palbociclib hydrochloride Description

Source:
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Storage:	Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C). Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com
After receiving:	The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.

Product Name	Palbociclib hydrochloride
Price:
CAS No.:	827022-32-2
Catalog No.:	CFN60047
Molecular Formula:	C₂₄H₂₉N₇O₂.HCl
Molecular Weight:	483.99 g/mol
Purity:	>=98%
Type of Compound:	Alkaloids
Physical Desc.:	Powder
Source:
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Download:	COA MSDS
Similar structural:	Comparison
Guestbook:

Size /Price /Stock	10 mM * 100 uL in DMSO / Inquiry / In-stock 10 mM * 1 mL in DMSO / Inquiry / In-stock
Related Libraries	Alkaloids Compound Library

	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	2.0662 mL	10.3308 mL	20.6616 mL	41.3232 mL	51.654 mL
5 mM	0.4132 mL	2.0662 mL	4.1323 mL	8.2646 mL	10.3308 mL
10 mM	0.2066 mL	1.0331 mL	2.0662 mL	4.1323 mL	5.1654 mL
50 mM	0.0413 mL	0.2066 mL	0.4132 mL	0.8265 mL	1.0331 mL
100 mM	0.0207 mL	0.1033 mL	0.2066 mL	0.4132 mL	0.5165 mL

CFN96440	Cauloside A	17184-21-3	604.81	C₃₅H₅₆O₈
CFN90882	Brandioside	133393-81-4	812.8	C₃₇H₄₈O₂₀
CFN93149	Ilexgenin A	108524-94-3	502.69	C₃₀H₄₆O₆
CFN97899	8-Prenylluteone	125002-91-7	422.5	C₂₅H₂₆O₆