Palbociclib isethionate | PD 0332991 isethionate | 帕布昔利布羟乙基磺酸盐 | CDK

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帕博西尼羟乙基磺酸盐 /Palbociclib isethionate 99%+

货号：A280869 同义名： 帕布昔利布羟乙基磺酸盐 / PD 0332991 isethionate

Palbociclib isethionate is a highly specific inhibitor of Cdk4 (IC50=11 nM) and Cdk6 (IC50=16 nM), having no activity against a panel of 36 additional protein kinases.

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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+

Palbociclib isethionate 化学结构
CAS号：827022-33-3

Palbociclib isethionate 3D分子结构
CAS号：827022-33-3

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Palbociclib isethionate 纯度/质量文件产品仅供科研

货号：A280869 标准纯度： 99%+ 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

CDK 亚型比较

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/CyclinE, IC50: 35 nM CDK2/CyclinA, IC50: 70 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	98%
JNJ-7706621		++++ CDK1/CyclinB, IC50: 9 nM		++++ CDK2/CyclinE, IC50: 3 nM CDK2/CyclinA, IC50: 4 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/CyclinE, IC50: 8 nM CDK2/CyclinA, 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/CyclinE, IC50: 363 nM CDK2/CyclinA, IC50: 45 nM		++ CDK4/CyclinD1, IC50: 160 nM	+ CDK5/p35, IC50: 265 nM		++ CDK7/CyclinH, IC50: 150 nM					99%+
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinE, IC50: 7.5μM CDK2/CyclinA, IC50: 0.68μM			+ CDK5/p35, IC50: 0.85μM							98%
SNS-032				+++ CDK2/CyclinE, IC50: 48 nM CDK2/CyclinA, IC50: 38 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	98%
(R)-Roscovitine	+ Cdc2/CyclinB, IC50: 0.65 μM			+ CDK2/CyclinE, IC50: 0.7 μM CDK2/CyclinA, 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/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 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/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 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				98+%
MSC2530818										++++ CDK8, IC50: 2.6 nM				99%+
Wogonin											✔			99%+
Riviciclib HCl		++ CDK1/CyclinB, IC50: 79 nM		+ CDK2/CyclinE, IC50: 2.54 μM CDK2/CyclinA, IC50: 224 nM		++ 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												++ Dyrk1B , IC50: 1648 nM CLK4, IC50: 136 nM		99%+
(E/Z)-TG003												+++ mCLK4, IC50: 15 nM mCLK1, IC50: 200 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。

Palbociclib isethionate 生物活性

靶点	CDK4 CDK4/CyclinD3, IC50:9 nM CDK4/CyclinD1, IC50:11 nM CDK6 CDK6/CyclinD2, IC50:15 nM
描述	CDK4/6, forming a complex with its partner Cyclin D1/2/3, can mediate the phosphorylation of Rb in G1 cell cycle, as well as stimulating the synthesis cyclin E and D-type cyclins controlled by extracellular mitogens^[1]. Palbociclib (PD 0332991) is a highly specific pyridopyrimidine-derived inhibitor of both CDK4 and CDK6 with IC50 values of 11 nM and 16 nM (measured by enzymatic activity), respectively. Treatment with 0.031 - 1 μM of palbociclib for 24h can decrease the level of Rb phosphorylation at Ser-780 in MDA-MB-435 human breast carcinoma cells. Palbociclib can potently inhibit cell growth in Rb-positive cells, such as MDA-MB-435, ZR-75-1, T-47D, MCF-7, H1299, Colo-205, CRRF-CEM and K562 cell lines, with IC50 values of 0.04 - 0.4 μM, as well as suppress DNA replication by preventing cells from entering S phase. Daily p.o. dosing for 14 days with palbociclib (150 or 75 mg/kg) can produce rapid tumor regressions in p16 deleted mice bearing Colo-205 colon carcinoma xenografts^[2]. Up to now, several phase 3 studies on Palbociclib of treatment for breast cancer are undergoing (see on https://www.clinicaltrials.gov/).
作用机制	Palbociclib can inhibit CDK4/6 in an ATP-competitive manner through its pyridopyrimidine structure.

Palbociclib isethionate 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
H157	0-100 μM	Growth Inhibition Assay	72 h	IC50=9 μM	26390342
H2170	0-100 μM	Growth Inhibition Assay	72 h	IC50=5 μM	26390342
H520	0-100 μM	Growth Inhibition Assay	72 h	IC50=0.73 μM	26390342
H596	0-100 μM	Growth Inhibition Assay	72 h	IC50=12 μM	26390342

Palbociclib isethionate 动物研究

Dose

Mice^[2] (p.o.): min = 12.5 mg/kg, max = 150 mg/kg

Administration

p.o.

Pharmacokinetics

Animal	Rats^[4]	Dogs^[4]	Monkeys^[4]
Dose	5 mg/kg (i.v.) 200 mg/kg (p.o.)	1.0 mg/kg (i.v.) 20 mg/kg (p.o.)	0.5 mg/kg (i.v.) 2.66 mg/kg (p.o.)
Administration	i.v. / p.o.	i.v. / p.o.	i.v. / p.o.
C_max	2507 ng/ml (i.v.) 2242 ng/ml (p.o.)	664 ± 247 ng/ml (p.o.)	86 ± 31 ng/ml (p.o.)
T_1/2	2.60 h (i.v.)	10.8 ± 0.3 h (i.v.) 20.7 ± 5.7 h (p.o.)	4.7 ± 1.4 h (i.v.) 5.3 ± 0.9 h (p.o.)
AUC_0→∞		2330 ± 258 ng·h/ml (i.v.)	624 ± 43 ng·h/ml (i.v.) 768 ± 150 ng·h/ml (p.o.)
AUC_0→t	2160 ng·hr/ml (i.v.) 76800 ng·hr/ml (p.o.)	1860 ± 222 ng·h/ml (i.v.) 17400 ± 6900 ng·h/ml (p.o.)
CL	37 ml/min/kg (i.v.)	7.22 ± 0.85 ml/min/kg (i.v.)	13.4 ± 0.9 ml/min/kg (i.v.)
T_max	0.08 h (i.v.) 30 h (p.o.)	8.7 ± 3.1 h (p.o.)	2.7 ± 1.2 h (p.o.)
F		36.9 ± 12.4 (%) (p.o.)	23.1 ± 3.6 (%) (p.o.)
V_d	7070 ml/kg (i.v.)
Vd_ss		6.2 ± 0.8 L/kg (i.v.)	5.1 ± 1.0 L/kg (i.v.)

Palbociclib isethionate 参考文献

[1]Roskoski R Jr, et al. Cyclin-dependent protein kinase inhibitors including palbociclib as anticancer drugs. Pharmacol Res. 2016 May;107:249-275.

[2]Fry DW, Harvey PJ, 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.

[3]Barvian M, Boschelli DH, et al. Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. J Med Chem. 2000 Nov 30;43(24):4606-16.

[4]207103Orig1s000PharmR

Palbociclib isethionate 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.74mL

0.35mL

0.17mL

8.72mL

1.74mL

0.87mL

17.43mL

3.49mL

1.74mL

Palbociclib isethionate 技术信息

CAS号	827022-33-3
分子式	C₂₆H₃₅N₇O₆S
分子量	573.664

别名	帕布昔利布羟乙基磺酸盐 ;PD 0332991 isethionate
运输	蓝冰

存储条件

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 9 mg/mL(15.69 mM)，配合低频超声助溶，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

H₂O: 50 mg/mL(87.16 mM)，配合低频超声助溶

动物实验配方

PO 0.5% CMC-Na 60 mg/mL suspension

H157	0-100 μM	Growth Inhibition Assay	72 h	IC50=9 μM	26390342
H2170	0-100 μM	Growth Inhibition Assay	72 h	IC50=5 μM	26390342
H520	0-100 μM	Growth Inhibition Assay	72 h	IC50=0.73 μM	26390342
H596	0-100 μM	Growth Inhibition Assay	72 h	IC50=12 μM	26390342
IMR-32		Growth Inhibition Assay	48 h	IC50=261 nM	26225123
IMR-32	1 μM	Growth Inhibition Assay	24 h	induces G1 arrest	26225123
IMR-32	0-1 μM	Fuction Assay	24 h	reduces the expression of TOP2A, CCNE2, and TK1 in a dose-dependent manner	26225123
MCF7	2.5-250 nM	Fuction Assay	24 h	reduces Rb phosphorylation	25991817
MOLM13	0.5 μM	Apoptosis Assay	24 h	enhances apoptosis induced by sorafenib and AC220	25487917
MOLM13-ITD alone		Growth Inhibition Assay		IC50=0.089 ± 0.009 μM	25487917
MOLM13-ITD/D835Y		Growth Inhibition Assay		IC50=0.114 ± 0.011 μM	25487917
MV4-11	0.5 μM	Apoptosis Assay	24 h	enhances apoptosis induced by sorafenib and AC220	25487917
MV4-11-ITD alone		Growth Inhibition Assay		IC50=0.092 ± 0.008 μM	25487917
MV4-11-ITD/D835V		Growth Inhibition Assay		IC50=0.116 ± 0.011 μM	25487917
MV4-11-ITD/D835V		Growth Inhibition Assay		IC50=0.102 ± 0.006 μM	25487917
MV4-11-ITD/F691L		Growth Inhibition Assay		IC50=0.112 ± 0.015 μM	25487917
MV4-11-ITD/N841K		Growth Inhibition Assay		IC50=0.113 ± 0.002 μM	25487917
NGP		Growth Inhibition Assay	48 h	IC50=2.077 μM	26225123
NGP	1 μM	Growth Inhibition Assay	24 h	induces G1 arrest	26225123
NGP	0-1 μM	Fuction Assay	24 h	reduces the expression of TOP2A, CCNE2, and TK1 in a dose-dependent manner	26225123
SH-EP		Growth Inhibition Assay	48 h	IC50=2.211 μM	26225123
SH-EP	1 μM	Growth Inhibition Assay	24 h	induces G1 arrest	26225123
SH-SY5Y		Growth Inhibition Assay	48 h	IC50=676 nM	26225123
SH-SY5Y	1 μM	Growth Inhibition Assay	24 h	induces G1 arrest	26225123
U937-FLT3 WT		Growth Inhibition Assay		IC50=0.102 ± 0.013 μM	25487917
U-CH11	0-1 μM	Growth Inhibition Assay	72 h	IC50=340 nM	26183925
U-CH2	0-1 μM	Growth Inhibition Assay	72 h	IC50=50.2 nM	26183925
U-CH3	0-1 μM	Growth Inhibition Assay	72 h	IC50=52 nM	26183925
U-CH6	0-1 μM	Growth Inhibition Assay	72 h	IC50=90 nM	26183925
U-CH7	0-1 μM	Growth Inhibition Assay	72 h	IC50=98 nM	26183925

帕博西尼羟乙基磺酸盐 /Palbociclib isethionate 99%+

Palbociclib isethionate 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Palbociclib isethionate 质控信息

Palbociclib isethionate 生物活性

Palbociclib isethionate 细胞研究

Palbociclib isethionate 动物研究

Palbociclib isethionate 参考文献

Palbociclib isethionate 实验方案

Palbociclib isethionate 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

热门区域

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CDK4	CDK4/CyclinD3, IC50:9 nM CDK4/CyclinD1, IC50:11 nM
CDK6	CDK6/CyclinD2, IC50:15 nM

帕博西尼羟乙基磺酸盐 /Palbociclib isethionate 99%+

Palbociclib isethionate 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Palbociclib isethionate 质控信息

Palbociclib isethionate 生物活性

Palbociclib isethionate 细胞研究

Palbociclib isethionate 动物研究

Palbociclib isethionate 参考文献

Palbociclib isethionate 实验方案

Palbociclib isethionate 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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热门区域

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B

C

F

G

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Palbociclib isethionate 纯度/质量文件产品仅供科研