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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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快速发货 顺丰冷链运输,1-2 天到达
品质保证
技术支持
免费溶解
产品名称 | Cdc ↓ ↑ | CDK1 ↓ ↑ | CDK19 ↓ ↑ | CDK2 ↓ ↑ | CDK3 ↓ ↑ | CDK4 ↓ ↑ | CDK5 ↓ ↑ | CDK6 ↓ ↑ | CDK7 ↓ ↑ | CDK8 ↓ ↑ | CDK9 ↓ ↑ | CLK ↓ ↑ | 其他靶点 | 纯度 | |||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
XL413 hydrochloride |
++++
Cdc7, IC50: 3.4 nM |
99%+ | |||||||||||||||||
SU9516 |
+++
CDK1, IC50: 40 nM |
+++
CDK2, IC50: 22 nM |
++
CDK4, IC50: 200 nM |
99%+ | |||||||||||||||
RO-3306 |
+++
CDK1, Ki: 20 nM |
SGK,ERK | 98% | ||||||||||||||||
R547 |
++++
CDK1/CyclinB, Ki: 2 nM |
++++
CDK2/CyclinE, Ki: 3 nM |
++++
CDK4/CyclinD1, Ki: 1 nM |
99%+ | |||||||||||||||
BMS-265246 |
++++
CDK1/CyclinB, IC50: 6 nM |
++++
CDK2/CyclinE, IC50: 9 nM |
+
CDK4/CyclinD, IC50: 230 nM |
99%+ | |||||||||||||||
NU6027 |
+
CDK1, Ki: 2.5 μM |
+
CDK2, Ki: 1.3 μM |
DNA-PK | 98% | |||||||||||||||
Purvalanol A |
++++
Cdc2/CyclinB, IC50: 4 nM |
+++
CDK2/CyclinA, IC50: 70 nM CDK2/CyclinE, IC50: 35 nM |
+
CDK4/CyclinD1, IC50: 850 nM |
99%+ | |||||||||||||||
SCH900776 |
++
CDK2, IC50: 0.16 μM |
99%+ | |||||||||||||||||
AUZ 454 |
++++
CDK2(A144C), Kd: 9.7 nM CDK2(C118L), Kd: 18.6 nM |
99%+ | |||||||||||||||||
A-674563 HCl |
++
CDK2, Ki: 46 nM |
PKA | 99% | ||||||||||||||||
JNJ-7706621 |
++++
CDK1/CyclinB, IC50: 9 nM |
++++
CDK2/CyclinA, IC50: 4 nM CDK2/CyclinE, IC50: 3 nM |
++
CDK3/CyclinE, IC50: 58 nM |
+
CDK4/CyclinD1, IC50: 253 nM |
++
CDK6/CyclinD1, IC50: 175 nM |
99%+ | |||||||||||||
AT7519 |
++
CDK1/CyclinB, IC50: 210 nM |
++
CDK2/CyclinA, IC50: 47 nM |
+
CDK3/CyclinE, IC50: 360 nM |
++
CDK4/CyclinD1, IC50: 100 nM |
+++
CDK5/p35, IC50: 13 nM |
++
CDK6/CyclinD3, IC50: 170 nM |
++++
CDK9/CyclinT, IC50: <10 nM |
98+% | |||||||||||
PHA-793887 |
++
CDK1/CyclinB, IC50: 60 nM |
++++
CDK2/CyclinA, IC50: 8 nM CDK2/CyclinE, IC50: 8 nM |
++
CDK4/CyclinD1, IC50: 62 nM |
++++
CDK5/p25, IC50: 5 nM |
++++
CDK7/CyclinH, IC50: 10 nM |
++
CDK9/CyclinT1, IC50: 138 nM |
99%+ | ||||||||||||
Milciclib |
+
CDK1/CyclinB, IC50: 398 nM |
++
CDK2/CyclinA, IC50: 45 nM CDK2/CyclinE, IC50: 363 nM |
++
CDK4/CyclinD1, IC50: 160 nM |
+
CDK5/p35, IC50: 265 nM |
++
CDK7/CyclinH, IC50: 150 nM |
99%+ | |||||||||||||
Kenpaullone |
+
CDK1/CyclinB, IC50: 0.4μM |
+
CDK2/CyclinA, IC50: 0.68μM CDK2/CyclinE, IC50: 7.5μM |
+
CDK5/p35, IC50: 0.85μM |
98% | |||||||||||||||
SNS-032 |
+++
CDK2/CyclinA, IC50: 38 nM CDK2/CyclinE, IC50: 48 nM |
+
CDK5/p35, IC50: 340 nM |
++
CDK7/CyclinH, IC50: 62 nM |
++++
CDK9/CyclinT, IC50: 4 nM |
99%+ | ||||||||||||||
Dinaciclib |
++++
CDK1, IC50: 3 nM |
++++
CDK2, IC50: 1 nM |
++++
CDK5, IC50: 1 nM |
++++
CDK9, IC50: 4 nM |
99%+ | ||||||||||||||
PHA-767491 hydrochloride |
++++
Cdc7, IC50: 10 nM |
+
CDK1, IC50: 250 nM |
+
CDK2, IC50: 240 nM |
+
CDK5, IC50: 460 nM |
+++
CDK9, IC50: 34 nM |
MK2 | 99% | ||||||||||||
(R)-Roscovitine |
+
Cdc2/CyclinB, IC50: 0.65 μM |
+
CDK2/CyclinA, IC50: 0.7 μM CDK2/CyclinE, IC50: 0.7 μM |
++
CDK5/p35, IC50: 0.16 μM |
99%+ | |||||||||||||||
Narazaciclib |
++++
CDK4/CyclinD1, IC50: 3.87 nM |
++++
CDK6/CyclinD1, IC50: 9.82 nM |
RET | 99%+ | |||||||||||||||
Palbociclib |
++++
CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM |
+++
CDK6/CyclinD2, IC50: 15 nM |
99% | ||||||||||||||||
Abemaciclib |
++++
CDK4, IC50: 2 nM |
++++
CDK6, IC50: 10 nM |
99% | ||||||||||||||||
Ribociclib |
++++
CDK4, IC50: 10 nM |
+++
CDK6, IC50: 39 nM |
98% | ||||||||||||||||
Palbociclib isethionate |
++++
CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM |
+++
CDK6/CyclinD2, IC50: 15 nM |
99%+ | ||||||||||||||||
BS-181 HCl |
+++
CDK7, IC50: 21 nM |
99%+ | |||||||||||||||||
(E/Z)-THZ1 dihydrochloride |
++++
CDK7, IC50: 3.2 nM |
99%+ | |||||||||||||||||
LDC4297 |
++++
CDK7, IC50: 0.13 nM |
99%+ | |||||||||||||||||
Senexin A |
+
CDK19, Kd: 0.31 μM |
+
CDK8, Kd: 0.83 μM |
99% | ||||||||||||||||
MSC2530818 |
++++
CDK8, IC50: 2.6 nM |
99%+ | |||||||||||||||||
Wogonin | ✔ | 99%+ | |||||||||||||||||
Riviciclib HCl |
++
CDK1/CyclinB, IC50: 79 nM |
+
CDK2/CyclinA, IC50: 224 nM CDK2/CyclinE, IC50: 2.54 μM |
++
CDK4/CyclinD1, IC50: 63 nM |
+
CDK6/CyclinD3, IC50: 396 nM |
+
CDK7/CyclinH, IC50: 2.87 μM |
+++
CDK9/CyclinT1, IC50: 20 nM |
99+% | ||||||||||||
LDC000067 |
+
CDK2, IC50: 2.441 μM |
++
CDK9, IC50: 44 nM |
98% | ||||||||||||||||
Flavopiridol |
+++
CDK1, IC50: 40 nM |
+++
CDK2, IC50: 40 nM |
+++
CDK4, IC50: 40 nM |
+++
CDK6, IC50: 40 nM |
+
CDK7, IC50: 300 nM |
+++
CDK9, IC50: 20 nM |
99%+ | ||||||||||||
LY2857785 |
+
CDK7, IC50: 0.246 μM |
+++
CDK8, IC50: 0.016 μM |
+++
CDK9, IC50: 0.011 μM |
99%+ | |||||||||||||||
AZD-5438 |
+++
CDK1, IC50: 16 nM |
++++
CDK2, IC50: 6 nM |
+++
CDK9, IC50: 20 nM |
99%+ | |||||||||||||||
ML167 |
++
CLK4, IC50: 136 nM Dyrk1B , IC50: 1648 nM |
99%+ | |||||||||||||||||
(E/Z)-TG003 |
+++
mCLK1, IC50: 200 nM mCLK4, IC50: 15 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | Palbociclib (PD 0332991) is an orally active, selective inhibitor of CDK4 and CDK6, showing IC50 values of 11 nM and 16 nM respectively. It exhibits strong anti-proliferative properties and is capable of inducing cell cycle arrest in cancer cells. This makes it a valuable agent in the study of HR-positive and HER2-negative breast cancer as well as hepatocellular carcinoma[1].[3].[4]. |
体内研究 | When administered orally at doses of 75 or 150 mg/kg daily for 14 days, Palbociclib leads to rapid tumor regressions and delays in tumor growth[1]. An oral dose of 90 mg/kg daily for 12 days decreases Treg numbers and the Treg:CD8 ratio in the spleen and lymph nodes of tumor-free mice, indicating its effects independent of tumors[2]. At a dose of 100 mg/kg administered daily for one week, Palbociclib demonstrates significant anti-tumor activity in a genetically engineered mosaic mouse model of liver cancer[4]. |
体外研究 | In laboratory tests, Palbociclib (0-1 μM, over 24 hours) inhibits Rb phosphorylation at Ser795 in MDA-MB-435 cells with an IC50 of 0.063 μM. It shows comparable effects on phosphorylation at both Ser780 and Ser795 in Colo-205 colon carcinoma cells[1]. Additionally, Palbociclib (0-10 μM, over 24 hours) specifically arrests MDA-MB-453 breast cancer cells in the G1 phase[1]. Over a period of 7 days, a 500 nM concentration of Palbociclib boosts the expression of homologous genes (H2d1, H2k1, and B2m) in MDA-MB-453 and MDA-MB-361 cells[2]. Palbociclib inhibits growth in various luminal ER-positive and HER2-amplified breast cancer cell lines when applied at concentrations from 0-1 μM for 6 days, with IC50 values ranging between 4 nM and 1 μM[3]. In human liver cancer cell lines, Palbociclib (0-1 μM, over 3 days) restricts proliferation with IC50 values from 0.01 μM to 3.49 μM and induces reversible cell cycle arrest[4]. |
作用机制 | Palbociclib can inhibit CDK4/6 in an ATP-competitive manner through its pyridopyrimidine structure[1][3][4]. |
Dose | Rat: 25 mg/kg[6] (i.p.); 1 mg/kg - 5 mg/kg[5] (i.v.) Mice: 100 mg/kg[7] (i.g., b.w.), 25 mg/kg - 125 mg/kg[8] (p.o.), 5 mg/kg - 200 mg/kg[5] (p.o.) | ||||||||||||||||||
Administration | i.p., i.g., p.o. | ||||||||||||||||||
Pharmacokinetics |
|
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT03007979 | Breast Cancer ... 展开 >> Breast Carcinoma Cancer of Breast Malignant Tumor of Breast 收起 << | Phase 2 | Recruiting | June 30, 2021 | United States, Missouri ... 展开 >> Washington University School of Medicine Recruiting Saint Louis, Missouri, United States, 63110 Contact: Cynthia X Ma, M.D., Ph.D. 314-362-9383 cynthiaxma@wustl.edu Principal Investigator: Cynthia X Ma, M.D., Ph.D. Sub-Investigator: Foluso O Ademuyiwa, M.D. Sub-Investigator: Ron Bose, M.D., Ph.D. Sub-Investigator: Mathew Cherian, M.D. Sub-Investigator: Ashley Frith, M.D. Sub-Investigator: Leonel Hernandez Aya, M.D. Sub-Investigator: Peter Oppelt, M.D. Sub-Investigator: Haeseong Park, M.D. Sub-Investigator: Caron Rigden, M.D. Sub-Investigator: Rama Suresh, M.D. Sub-Investigator: Katherine Weilbaecher, M.D. Sub-Investigator: Rebecca Aft, M.D., Ph.D. Sub-Investigator: Lindsay Peterson, M.D. United States, Nebraska University of Nebraska Recruiting Lincoln, Nebraska, United States, 68588 Contact: Jairam Krishnamurthy, M.D. 402-559-1800 jairam.krishnamurthy@unmc.edu Principal Investigator: Jairam Krishnamurthy, M.D. Sub-Investigator: Kenneth Cowan, M.D. Sub-Investigator: Elizabeth Reed, M.D. Sub-Investigator: Pavankumar Tandra, M.D. 收起 << |
NCT01907607 | Advanced Gastrointestinal Stro... 展开 >>mal Tumors 收起 << | Phase 2 | Active, not recruiting | April 2019 | France ... 展开 >> Institut Bergonié Bordeaux, Gironde, France, 33076 Centre Georges-Francois Leclerc Dijon, France, 21079 Centre Oscar Lambret Lille, France, 59020 Centre Léon Bérard Lyon, France, 69373 Hôpital de la Timone - AP-HM Marseille, France, 13385 Centre René Gauducheau Nantes, France, 44805 Hôpital Saint-Antoine (AP-HP) Paris, France, 75571 CHU de REIMS - Hôpital Robert Debré Reims, France, 51092 Institut Gustave Roussy Villejuif, France, 94800 收起 << |
NCT03304080 | Breast Neoplasms ... 展开 >> Breast Diseases 收起 << | Phase 1 Phase 2 | Recruiting | November 1, 2019 | United States, New York ... 展开 >> Mount Sinai Beth Israel Comprehensive Cancer Center West Recruiting New York, New York, United States, 10011 Contact: Paula Klein, MD 212-604-6021 paula.klein@mountsinai.org Perlmutter Cancer Center NYU Langone Not yet recruiting New York, New York, United States, 10016 Contact: Sylvia Adams, MD 212-731-5795 sylvia.adams@nyumc.org Sub-Investigator: Sylvia Adams, MD Mount Sinai West Recruiting New York, New York, United States, 10019 Contact: Krystal Cascetta, MD 212-523-8692 krystal.cascetta@mountsinai.org New York Presbyterian Herbert Irving Comprehensive Cancer Center at Columbia University Not yet recruiting New York, New York, United States, 10032 Contact: Kevin Kalinsky, MD 212-305-1945 Kk2693@columbia.edu New York Presbyterian Meyer Cancer Center at Weill Cornell Not yet recruiting New York, New York, United States, 10065 Contact: Eleni Andreopoulou, MD 646-962-9888 ela9082@med.cornell.edu 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.23mL 0.45mL 0.22mL |
11.17mL 2.23mL 1.12mL |
22.34mL 4.47mL 2.23mL |
CAS号 | 571190-30-2 |
分子式 | C24H29N7O2 |
分子量 | 447.533 |
别名 | 帕布昔利布 ;PD 0332991 |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,Room Temperature |
溶解度 |
DMSO: 10 mg/mL(22.34 mM),配合低频超声,水浴加热至45℃,并调节pH至4,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 0.1 M HCL: 25 mg/mL(55.86 mM),配合低频超声,并调节pH至4 |
动物实验配方 |