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CAS No. : 571189-11-2
MCE 国际站：Palbociclib hydrochloride
产品活性：Palbociclib (PD 0332991) hydrochloride 是一种具有口服活性的 CDK4 和 CDK6 选择性抑制剂，IC50 值分别为 11 nM 和16 nM。Palbociclib hydrochloride 对癌细胞具有抗增殖活▓性，并诱导其细胞周期阻滞，可用于 HR 阳性和 HER2 阴性乳腺癌，以及肝细胞癌的相关研究。
作用靶点：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.
相关产品：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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