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CAS No. : 571189-11-2

MCE 國際站：Palbociclib hydrochloride

產(chǎn)品活性：Palbociclib (PD 0332991) hydrochloride 是一種具有口服活性的 CDK4 和 CDK6 選擇性抑制劑，IC₅₀ 值分別為 11 nM 和16 nM。Palbociclib hydrochloride 對(duì)癌細(xì)胞具有抗增殖活性，并誘導(dǎo)其細(xì)胞周期阻滯，可用于 HR 陽性和 HER2 陰性乳腺癌，以及肝細(xì)胞癌的相關(guān)研究。

研究領(lǐng)域：Cell Cycle/DNA Damage

作用靶點(diǎn)：CDK

In Vitro: Palbociclib (0-1 μM, 24 h) hydrochloride inhibits retinoblastoma 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 (0-10 μM, 24 h) hydrochloride arrests MDA-MB-453 cells exclusively in G1 phase.
Palbociclib (500 nM, 7 days) hydrochloride increases expression of homologous genes (H2d1, H2k1, and B2m) in MDA-MB-453 and MDA-MB-361 cells.
Palbociclib (0-1 μM, 6 days) hydrochloride 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 (0-1 μM, 3 days) hydrochloride 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 (oral adminstration, 75 or 150 mg/kg, daily for 14 days) hydrochloride produces rapid tumor regressions and delays tumor growth.
Palbociclib (oral adminstration, 90 mg/kg, daily for 12 days) hydrochloride reduces Treg numbers and the Treg:CD8 ratio in the spleen and lymph nodes in tumor-free mice, demonstrating the tumor-independent effects.
Palbociclib (oral administration, 100 mg/kg, daily for 1 week) hydrochloride has potent antitumour effects in genetically engineered mosaic mouse model of liver cancer.

相關(guān)產(chǎn)品：SY-5609  |  CLK1/2-IN-1  |  SB-218078  |  Toyocamycin  |  (S)-LY3177833 hydrate  |  Dinaciclib  |  EGFR/HER2/CDK9-IN-2  |  CDK8-IN-11  |  SNS-032  |  M2N12  |  Palbociclib-d8  |  BSJ-04-132  |  (E/Z)-Zotiraciclib  |  CCT-251921  |  BS-181  |  CDK9-IN-9  |  Flavopiridol  |  SRI-29329  |  dCeMM4  |  GSK 3 Inhibitor IX  |  CDK9-IN-7  |  BSJ-03-204  |  K00546  |  Abemaciclib metabolite M18 hydrochloride  |  Ribociclib-d6  |  Lacto-N-fucopentaose I  |  CDK12-IN-2  |  BSJ-03-123  |  CLK-IN-T3N  |  IV-361

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