PHA-793887 | CDK Inhibitor | AmBeed-信号通路专用抑制剂

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PHA-793887 {[allProObj[0].p_purity_real_show]}

货号：A184364

PHA-793887 is a pan-cdk inhibitor, inhibits cdk1/2/4/5/7/9 with IC50s of 5 - 140 nM.

PHA-793887 化学结构
CAS号：718630-59-2

PHA-793887 3D分子结构
CAS号：718630-59-2

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PHA-793887 纯度/质量文件产品仅供科研

货号：A184364 标准纯度： {[allProObj[0].p_purity_real_show]} 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, 101755. Ambeed. [ A399663 ]; • EMBO J., 2024. Ambeed. [ A295334 ]; • JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]; • JMC, 2024. Ambeed. [ A210558 , A1518164 ]; • Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]; 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											ERK,SGK	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(C118L), Kd: 18.6 nM CDK2(A144C), Kd: 9.7 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												++ 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。

PHA-793887 生物活性

靶点	CDK5 CDK5/p25, IC50:5 nM CDK4 CDK4/CyclinD1, IC50:62 nM CDK2 CDK2/CyclinE, IC50:8 nM CDK2/CyclinA, IC50:8 nM CDK9 CDK9/CyclinT1, IC50:138 nM
描述	Cyclin dependent kinases (CDKs) are a family of serine/threonine kinases that, in concert with cyclins (positive regulators) and natural inhibitors (CDKI), control the cell cycle progression. PHA -793887 is a novel and effective CDK2, CDK5 and CDK7 inhibitor with IC₅₀ of 8 nM, 5 nM and 10 nM, respectively. A2780 ovarian carcinoma cells were treated with PHA-793887 for 24 h at the concentration of 3 μM and 1 μM. A decrease in the S phase population and a subsequent increase of the G1 population, as expected for inhibition of CDK2/cyclin A, were observed at 1 μM treatment compared to the control cells. At 3 μM only a strong G2/M increase was observed, which can be ascribed to inhibition of CDK1/cyclin B. The presence of cells with sub G1 DNA content (from 2.6% in control cells to 26.2% in cells treated with PHA-793887 at 3 μM) clearly implied cell death and apoptosis. A clear reduction in DNA synthesis was observed, compared to the control group. A clear reduction of the hyperphosphorylated form of pRb (retinoblastoma protein, a known CDK substrate) and an accumulation of the hypophosphorylated form of pRb were observed in the extracts of treated cell. PHA-793887 (1 or 3 μM) decreases the amount of pRB (retinoblastoma protein, a known CDK substrate) phosphorylation in treated cells in comparison with untreated cells. PHA-793887 caused a dose-dependent inhibition of the A2780 tumor growth up to 76% at the dose of 30 mg/kg in the human ovarian A2780 xenograft mouse model^[4].
作用机制	The pyrrolo-pyrazole system of PHA-793887 occupies the adenine region of the ATP pocket, while the iso-butyl group points towards the solvent accessible region.

PHA-793887 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
human A2780 cells		Proliferation assay	72 h	Antiproliferative activity against human A2780 cells after 72 hrs by fluorescence assay, IC50=0.09 μM	20153204
human A2780 cells	3 μM	Function assay		Inhibition of CDK in human A2780 cells assessed as accumulation of hypophosphorylated form of retinoblastoma protein at 3 uM by immunohistochemistry	20153204
human A375 cells		Proliferation assay	72 h	Antiproliferative activity against human A375 cells after 72 hrs by SRB assay, IC50=0.396 μM	20153204
human BxPC3 cells		Proliferation assay	72 h	Antiproliferative activity against human BxPC3 cells after 72 hrs by SRB assay, IC50=3.444 μM	20153204

PHA-793887 动物研究

Dose

CD-1 nude mice: 15 mg/kg, 30 mg/kg^[3] (i.v.)

Administration

i.v.

Pharmacokinetics

Animal	Nude mice^[1]
Dose	10 mg/kg
Administration	i.v.
T_1/2	4.1 h
AUC	19.2 μM·h
CL	23.9 ml/min/kg
C_max	36.5 μM
V_ss	1360 ml/kg

PHA-793887 参考文献

[1]Brasca MG, Albanese C, et al. Optimization of 6,6-dimethyl pyrrolo[3,4-c] pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing. Bioorg Med Chem. 2010 Mar 1;18(5):1844-53.

[2]Alzani R, Pedrini O, et al. Therapeutic efficacy of the pan-cdk inhibitor PHA-793887 in vitro and in vivo in engraftment and high-burden leukemia models. Exp Hematol. 2010 Apr;38(4):259-269.e2.

[3]Locatelli G, Bosotti R, et al. Transcriptional analysis of an E2F gene signature as a biomarker of activity of the cyclin-dependent kinase inhibitor PHA-793887 in tumor and skin biopsies from a phase I clinical study. Mol Cancer Ther. 2010 May;9(5):1265-73.

[4]Brasca MG, Albanese C, Alzani R, Amici R, Avanzi N, Ballinari D, Bischoff J, Borghi D, Casale E, Croci V, Fiorentini F, Isacchi A, Mercurio C, Nesi M, Orsini P, Pastori W, Pesenti E, Pevarello P, Roussel P, Varasi M, Volpi D, Vulpetti A, Ciomei M. Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing. Bioorg Med Chem. 2010 Mar 1;18(5):1844-53. doi: 10.1016/j.bmc.2010.01.042. Epub 2010 Jan 25. PMID: 20153204.

PHA-793887 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.77mL

0.55mL

0.28mL

13.83mL

2.77mL

1.38mL

27.66mL

5.53mL

2.77mL

PHA-793887 技术信息

CAS号	718630-59-2
分子式	C₁₉H₃₁N₅O₂
分子量	361.482

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 50 mg/mL(138.32 mM)，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

动物实验配方

IP 2% DMSO+2% Tween80+30% PEG300+water 10 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

PHA-793887 {[allProObj[0].p_purity_real_show]}

PHA-793887 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

PHA-793887 质控信息

PHA-793887 生物活性

PHA-793887 细胞研究

PHA-793887 动物研究

PHA-793887 参考文献

PHA-793887 实验方案

PHA-793887 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

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CDK5	CDK5/p25, IC50:5 nM
CDK4	CDK4/CyclinD1, IC50:62 nM
CDK2	CDK2/CyclinE, IC50:8 nM CDK2/CyclinA, IC50:8 nM
CDK9	CDK9/CyclinT1, IC50:138 nM
CDK7	CDK7/CyclinH, IC50:10 nM
CDK1	CDK1/CyclinB, IC50:60 nM

PHA-793887 {[allProObj[0].p_purity_real_show]}

PHA-793887 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

PHA-793887 质控信息

PHA-793887 生物活性

PHA-793887 细胞研究

PHA-793887 动物研究

PHA-793887 参考文献

PHA-793887 实验方案

PHA-793887 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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PHA-793887 纯度/质量文件产品仅供科研