ARO 002
Crenolanib
CAS: 670220-88-9
Molecular Formula: C26H29N5O2
ARO 002 - Names and Identifiers
ARO 002 - Physico-chemical Properties
| Molecular Formula | C26H29N5O2 |
| Molar Mass | 443.54 |
| Density | 1.36 |
| Boling Point | 676.6±65.0 °C(Predicted) |
| Solubility | Soluble in DMSO, not in water |
| Appearance | solid |
| Color | White |
| pKa | 9.84±0.20(Predicted) |
| Storage Condition | -20° |
| Stability | Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month. |
| Use | Crenolanib is an effective and selective wild-type and mutant type III receptor tyrosine kinase inhibitor, the Kd of inhibiting FLT3 and PDGFRα/β is 0.74 nM,2.1 nM,3.2 nM, respectively. |
| In vitro study | Crenolanib is significantly more potent than imatinib in inhibiting the kinase activity of imatinib-resistant PDGFRα kinases (D842I, D842V, D842Y, D1842-843IM, and deletion I843). Crenolanib is 135-fold more otent than imatinib against D842V in the isogenic model system with an IC50 of approximately 10 nM. Crenolanib inhibits the kinase activity of the fusion oncogene in EOL-1 cell line, which is derived from a patient with chronic eosinophilic leukemia and expresses the constitutively activated FIP1L1- PDGFRα fusion kinase with IC50 = 21 nM. Crenolanib also inhibits the proliferation of EOL-1 cells with IC50 = 0.2 pM. Crenolanib inhibits the activation of V561D or D842V-mutant kinases expressed in BaF3 cells with IC50 with 85 nM or 272 nM, respectively. Crenolanib inhibits PDGFRα activation in H1703 non-small cell lung cancer cell line which has 24-fold amplification of the 4q12 region that contains the PDGFRα locus, with IC50 with 26 nM. Crenolanib is an orally bioavailable, high ly pot and selective PDGFR TKI. Crenolainb is a benzidazole compound that has IC50s of 0.9 nM and 1.8 nM for PDGFRA and PDGFRB, review. The activity of imatinib-resistant PDGFRα kinase (D842I, 42v, D842Y,D1842-843IM, and deletion I843) was significantly more potent than that of imatinib. Crenolinib is 135 times more potent than imatinib for D842V in the syngeneic model system, with an IC50 of approximately 10 nM. Crenolanyl B inhibits the kinase activity of oncogenic fusion genes in EOL-1 cells, which is derived from patients with chronic acidophage leukemia and expresses a persistently activated FIP1L1- PDGFRα fusion kinase with IC50 = 21 nM. Crenolinib also inhibited cell proliferation by EOL-1 with IC50 = 0.2 pM. Crenolinib inhibited the activation of V561D or D842V mutant kinases expressed in BaF3 cells with an IC50 of 85 nM or 272 nM, respectively. Crenolanyl B inhibits PDGFRα activation in the H1703 non-small cell lung cancer cell line, which is capable of amplifying the 4q12 region containing the PDGFRα locus 24-fold with an IC50 of 26 nM. Crenolanyl B is an oral biologically active, highly potent, selective PDGFR TKI. Crenolanyl B is a benzimidazole compound with IC50s of 0.9 nM and 1.8 nM for PDGFRA and PDGFRB, respectively. |
ARO 002 - Reference
| Reference Show more | 1: Michael M, Vlahovic G, Khamly K, Pierce KJ, Guo F, Olszanski AJ. Phase Ib study of CP-868,596, a PDGFR inhibitor, combined with docetaxel with or without axitinib, a VEGFR inhibitor. Br J Cancer. 2010 Nov 9;103(10):1554-61. Epub 2010 Oct 19. PubMed PMID: 20959830; PubMed Central PMCID: PMC2990584. 2: Lewis NL, Lewis LD, Eder JP, Reddy NJ, Guo F, Pierce KJ, Olszanski AJ, Cohen RB. Phase I study of the safety, tolerability, and pharmacokinetics of oral CP-868,596, a highly specific platelet-derived growth factor receptor tyrosine kinase inhibitor in patients with advanced cancers. J Clin Oncol. 2009 Nov 1;27(31):5262-9. Epub 2009 Sep 8. PubMed PMID: 19738123; PubMed Central PMCID: PMC2773478. |
ARO 002 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.255 ml | 11.273 ml | 22.546 ml |
| 5 mM | 0.451 ml | 2.255 ml | 4.509 ml |
| 10 mM | 0.225 ml | 1.127 ml | 2.255 ml |
| 5 mM | 0.045 ml | 0.225 ml | 0.451 ml |
Last Update：2024-01-02 23:10:35
ARO 002 - Introduction
Crenolanib is an organic compound with the chemical formula C26H27N5O2 and a molecular weight of 441.52g/mol.
The compound has the following properties:
-Appearance: Colorless to light yellow solid
-Melting point: About 156-163 degrees Celsius
-Solubility: Slightly soluble in water, soluble in organic solvents such as chloroform, dimethyl sulfoxide and ether
Crenolanib has important applications in the field of medicine, and is often used as an intermediate for anti-tumor drugs, such as the synthesis of anti-breast cancer drugs.
The method of preparing Crenolanib can be synthesized through a multi-step reaction, and the specific synthesis route will vary according to the structure of the compound and the change of reaction conditions.
During use and handling, you need to pay attention to the safety information of the compound:
-The substance may cause irritation and damage to the human body. Appropriate safety measures should be taken, such as wearing protective gloves and safety glasses, and ensuring good ventilation.
-Avoid inhaling dust, contact with skin and eyes, if accidental contact, rinse immediately with plenty of water.
-Avoid high temperatures, fire sources and oxidants during storage, and ensure that the container is sealed to avoid contact with air, moisture and light.
-Observe local regulations when disposing of waste and treat it as hazardous waste.
The compound has the following properties:
-Appearance: Colorless to light yellow solid
-Melting point: About 156-163 degrees Celsius
-Solubility: Slightly soluble in water, soluble in organic solvents such as chloroform, dimethyl sulfoxide and ether
Crenolanib has important applications in the field of medicine, and is often used as an intermediate for anti-tumor drugs, such as the synthesis of anti-breast cancer drugs.
The method of preparing Crenolanib can be synthesized through a multi-step reaction, and the specific synthesis route will vary according to the structure of the compound and the change of reaction conditions.
During use and handling, you need to pay attention to the safety information of the compound:
-The substance may cause irritation and damage to the human body. Appropriate safety measures should be taken, such as wearing protective gloves and safety glasses, and ensuring good ventilation.
-Avoid inhaling dust, contact with skin and eyes, if accidental contact, rinse immediately with plenty of water.
-Avoid high temperatures, fire sources and oxidants during storage, and ensure that the container is sealed to avoid contact with air, moisture and light.
-Observe local regulations when disposing of waste and treat it as hazardous waste.
Last Update：2024-04-09 21:21:28
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Product Name: Crenolanib (CP-868596) Visit Supplier Webpage Request for quotationCAS: 670220-88-9
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Mobile: 18021002903
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Spot supply
Product Name: Crenolanib (CP-868596) Visit Supplier Webpage Request for quotationCAS: 670220-88-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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