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CAS No.: 670220-88-9

Crenolanib/克莱拉尼 Catalog No. CSN12987

Synonyms: CP-868596;ARO 002;CP 868,596

Crenolanib is a potent class III RTKs inhibitor with Kd values of 3.2nM, 2.1nM and 0.74nM for PDGFRα, PDGFRβ and FLT3.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 PDGFRα

Kd:2.1nM PDGFRβ

Kd:3.2nM
描述The activating mutations of KIT or PDGFRα are important to the pathogenesis of tumors. Crenolanib is a potent class III RTKs inhibitor with Kd values of 3.2nM, 2.1nM and 0.74nM for PDGFRα, PDGFRβ and FLT3 (measured by Kd ELECT screening service), respectively, as well as showed kinase inhibition effect on imatinib-resistant mutation including PDGFRA D842I, D842V, D842Y and DI842-843IM in CHO cells transfected with PDGFRA constructs. Consistent with this, Crenolanib inhibited cell proliferation more potently than imatinib in BaF3 expressed PDGFRA-D842V mutation cells at concentration>50nM^[1]. As the potent inhibition by Crenolanib to FLT3, Crenolanib at concentration ranging in 1-50nM dose-dependently inhibited FLT3-ITD AML cell viability and FLT3 signaling, shown as decreased phosphorylation of –FLT3, STAT5, ERK and S6, in MV4-11 and MOLM-13 cells. Administration of Crenolanib at dose of 15mg/kg twice daily (Monday to Friday) for 3 consecutive weeks significantly reduced MOLM-13-RES-luc leukemic infiltration and produce a significant increase in survival in NSG mice engrafted with MOLM-13-RES-luc cells^[2].
作用机制Crenolanib is an selective ATP-competitive inhibitor of class III RTKs, PDGFRα, PDGFRβ and FLT3.^[3]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
A549	0-1000 nM	Growth Inhibition Assay	24/48/72 h	inhibits cell growth dose and time dependently	25328409
A549	500 nM	Apoptosis Assay	48 h	induces cell apoptosis	25328409
A549	12.5/25/50 nM	Function Assay	10 h	inhibits cell migration	25328409

更多
动物研究
剂量
Mice: 5 mg/kg^[3] (p.o.)

给药途径
p.o.
参考文献

动物研究
剂量	Mice: 5 mg/kg^[3] (p.o.)
给药途径	p.o.

[1] Heinrich MC, Griffith D, et al. Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors. Clin Cancer Res. 2012 Aug 15;18(16):4375-84.
[2] Zimmerman EI, Turner DC, et al. Crenolanib is active against models of drug-resistant FLT3-ITD-positive acute myeloid leukemia. Blood. 2013 Nov 21;122(22):3607-15.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2546 mL
- 11.2729 mL
- 22.5459 mL
- 5 mM
- 0.4509 mL
- 2.2546 mL
- 4.5092 mL
- 10 mM
- 0.2255 mL
- 1.1273 mL
- 2.2546 mL

技术信息

CAS号

670220-88-9

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H29N5O2

运输

蓝冰

分子量

443.54

别名

CP-868596;ARO 002;CP 868,596;RO-002

溶解度

DMSO	86.0 mg/mL (193.9 mM) warming
Water	Insoluble
Ethanol	7.0 mg/mL (15.8 mM)

动物实验配方

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

A549	0-1000 nM	Growth Inhibition Assay	24/48/72 h	inhibits cell growth dose and time dependently	25328409
A549	500 nM	Apoptosis Assay	48 h	induces cell apoptosis	25328409
A549	12.5/25/50 nM	Function Assay	10 h	inhibits cell migration	25328409
Ba/F3 ITD	-	Growth Inhibition Assay	-	IC50=1.3 μM	24227820
Ba/F3 ITD/D835Y	-	Growth Inhibition Assay	-	IC50=8.7 μM	24227820
Ba/F3 ITD/F691L	-	Growth Inhibition Assay	-	IC50=67.8 μM	24227820
Ba/F3 WT D835F	-	Growth Inhibition Assay	-	IC50=6.5 μM	24227820
Ba/F3 WT D835H	-	Growth Inhibition Assay	-	IC50=19.8 μM	24227820
Ba/F3 WT D835N	-	Growth Inhibition Assay	-	IC50=4.3 μM	24227820
Ba/F3 WT D835V	-	Growth Inhibition Assay	-	IC50=2.3 μM	24227820
Ba/F3 WT D835Y	-	Growth Inhibition Assay	-	IC50=6.9 μM	24227820
HL60	-	Growth Inhibition Assay	-	IC50=1±0.03 μM	25597754
HL60	-	Growth Inhibition Assay	-	IC50=1.46±0.04 μM	25597754
HL60	-	Growth Inhibition Assay	-	IC50=0.86±0.02 μM	25597754
HL60/ADR	-	Growth Inhibition Assay	-	IC50=1.72±0.06 μM	25597754
HL60/VCR	-	Growth Inhibition Assay	-	IC50=6.93±0.03 μM	25597754
HL60/VCR	-	Growth Inhibition Assay	-	IC50=6.27±0.02 μM	25597754
HL60/VCR+PSC-833	-	Growth Inhibition Assay	-	IC50=0.84±0.04 μM	25597754
HL60+PSC-833	-	Growth Inhibition Assay	-	IC50=1.32±0.06 μM	25597754
K562	-	Growth Inhibition Assay	-	IC50=1.3±0.03 μM	25597754
K562	-	Growth Inhibition Assay	-	IC50=2.02±0.05 μM	25597754
K562/ABCB1	-	Growth Inhibition Assay	-	IC50=4.67±0.01 μM	25597754
K562/ABCB1	-	Growth Inhibition Assay	-	IC50=4.49±0.04 μM	25597754
K562/ABCB1+PSC-833	-	Growth Inhibition Assay	-	IC50=2.06±0.08 μM	25597754
K562/ABCG2	-	Growth Inhibition Assay	-	IC50=1.54±0.03 μM	25597754
K562+PSC-833	-	Growth Inhibition Assay	-	IC50=2.02±0.08 μM	25597754
M21	1 μM	Apoptosis Assay	24 h	induces cell apoptosis significantly combined with vemurafenib	24732172
M21R	1 μM	Apoptosis Assay	24 h	induces cell apoptosis significantly combined with vemurafenib	24732172
MOLM-13	0-1 μM	Cell Viablity Assay	72 h	inhibits cell viability dose dependently	24046014
MV4-11	0-1 μM	Cell Viablity Assay	72 h	inhibits cell viability dose dependently	24046014
OCI-AML3	0-100 μM	Cell Viablity Assay	72 h	inhibits cell viability dose dependently	24046014
PL21	0-100 μM	Cell Viablity Assay	72 h	inhibits cell viability dose dependently	24046014
THP-1	0-100 μM	Cell Viablity Assay	72 h	inhibits cell viability dose dependently	24046014
TPF-10-741	1 μM	Apoptosis Assay	24 h	induces cell apoptosis significantly combined with vemurafenib	24732172
U937	0-100 μM	Cell Viablity Assay	72 h	inhibits cell viability dose dependently	24046014

靶点	Description	IC50
PDGFRα		Kd:2.1nM
PDGFRβ		Kd:3.2nM

Crenolanib/克莱拉尼 Catalog No. CSN12987

靶点选择性

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