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CAS No.: 670220-88-9
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.
生物活性
靶点 | PDGFRα Kd:2.1nM | PDGFRβ Kd:3.2nM |
动物研究 | |
剂量 | Mice: 5 mg/kg[3] (p.o.) |
给药途径 | p.o. |
实验方案
技术信息
CAS号 | 670220-88-9 | 储存条件 |
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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 |
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动物实验配方 |
Cell Lines | Concentration | Assay Type | Time | Activity Description | Data Sources |
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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 |
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PDGFRα | Kd:2.1nM | |
PDGFRβ | Kd:3.2nM |
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