Palbociclib Isethionate free base

Palbociclib isethionate is an orally active selective CDK4 and CDK6 inhibitor.

For research use only. Not for human or veterinary use.

Target CDK

Research area Infection Neurological Disease Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

Palbociclib Isethionate structure

CAS No.: 827022-33-3

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
1 g	USD 448.00	BP-02086-1g	In stock	Get quote
2 g	USD 716.00	BP-02086-2g	In stock	Get quote
3 g	USD 860.00	BP-02086-3g	In stock	Get quote
5 g	USD 1,145.00	BP-02086-5g	In stock	Get quote
10 g	USD 1,835.00	BP-02086-10g	In stock	Get quote
25 g	USD 3,670.00	BP-02086-25g	In stock	Get quote

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Description

Palbociclib (PD 0332991) isethionate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib isethionate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.

Biological activity

In Vitro Palbociclib dihydrochloride (0-1 μM, 24 h) inhibits Rb Phosphorylation at Ser795 in MDA-MB-435 cells with an IC50 value of 0.063 μM, and obtains similar effects on both Ser780 and Ser795 phosphorylation in the Colo-205 colon carcinoma. Palbociclib dihydrochloride (0-10 μM, 24 h) arrests MDA-MB-453 cells exclusively in G1 phase. Palbociclib dihydrochloride (500 nM, 7 days) increases expression of homologous genes (H2d1, H2k1, and B2m) in MDA-MB-453 and MDA-MB-361 cells. Palbociclib dihydrochloride (0-1 μM, 6 days) inhibits growth of several luminal ER-positive as well as HER2-amplified breast cancer cell lines, with IC50 values ranging from 4 nM to 1 μM. Palbociclib dihydrochloride (0-1 μM, 3 days) inhibits the proliferation of human liver cancer cell lines with IC50 values ranging from 0.01 μM to 3.49 μM, and induces a reversible cell cycle arrest. In Vivo Palbociclib isethionate (oral adminstration, 75 or 150 mg/kg, daily for 14 days) produces rapid tumor regressions and delays tumor growth. Palbociclib isethionate (oral adminstration, 90 mg/kg, daily for 12 days) reduces Treg numbers and the Treg:CD8 ratio in the spleen and lymph nodes in tumor-free mice, demonstrating the tumor-independent effects. Palbociclib isethionate (oral administration, 100 mg/kg, daily for 1 week) has potent antitumour effects in genetically engineered mosaic mouse model of liver cancer.

Identifiers

SMILES: CC1=C(C(C)=O)C(N(C2CCCC2)C3=NC(NC4=NC=C(N5CCNCC5)C=C4)=NC=C13)=O.O=S(CCO)(O)=O
InChIKey: LYYVFHRFIJKPOV-UHFFFAOYSA-N

Specifications

MW (average): 573.6640
Formula: C₂₆H₃₅N₇O₆S
CAS No.: 827022-33-3
Physical state: Solid
Color: Light yellow to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder 4°C, sealed storage, away from moisture; In solvent -20℃ 1 month;

Solubility

Soluble in H2O 50 mg/mL DMSO 10 mg/mL

Documents

References

[1]. Fry DW, et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004 Nov;3(11):1427-38.

[2]. Goel S, et al. CDK4/6 inhibition triggers anti-tumour immunity. Nature. 2017 Aug 24;548(7668):471-475.

[3]. Richard S Finn, et al. PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro. Breast Cancer Res. 2009;11(5):R77.

[4]. Bollard J, et al. Palbociclib (PD-0332991), a selective CDK4/6 inhibitor, restricts tumour growth in preclinical models of hepatocellular carcinoma. Gut. 2017 Jul;66(7):1286-1296.

Same target

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Same research area

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