Crenolanib (CP-868596)PDGFR-β inhibitor,potent and selective CAS# 670220-88-9 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 670220-88-9 | SDF | Download SDF |
PubChem ID | 10366136 | Appearance | Powder |
Formula | C26H29N5O2 | M.Wt | 443.54 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Synonyms | CP-868596 | ||
Solubility | DMSO : 33.33 mg/mL (75.15 mM; Need ultrasonic) | ||
Chemical Name | 1-[2-[5-[(3-methyloxetan-3-yl)methoxy]benzimidazol-1-yl]quinolin-8-yl]piperidin-4-amine | ||
SMILES | CC1(COC1)COC2=CC3=C(C=C2)N(C=N3)C4=NC5=C(C=CC=C5N6CCC(CC6)N)C=C4 | ||
Standard InChIKey | DYNHJHQFHQTFTP-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C26H29N5O2/c1-26(14-32-15-26)16-33-20-6-7-22-21(13-20)28-17-31(22)24-8-5-18-3-2-4-23(25(18)29-24)30-11-9-19(27)10-12-30/h2-8,13,17,19H,9-12,14-16,27H2,1H3 | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | Crenolanib (CP-868596) is a potent and selective inhibitor of PDGFRα/β with Kd of 2.1 nM/3.2 nM. | |||||
Targets | PDGFRα | PDGFRβ | ||||
IC50 | 2.1 nM (Kd) | 3.2 nM (Kd) |
Crenolanib (CP-868596) Dilution Calculator
Crenolanib (CP-868596) Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.2546 mL | 11.2729 mL | 22.5459 mL | 45.0918 mL | 56.3647 mL |
5 mM | 0.4509 mL | 2.2546 mL | 4.5092 mL | 9.0184 mL | 11.2729 mL |
10 mM | 0.2255 mL | 1.1273 mL | 2.2546 mL | 4.5092 mL | 5.6365 mL |
50 mM | 0.0451 mL | 0.2255 mL | 0.4509 mL | 0.9018 mL | 1.1273 mL |
100 mM | 0.0225 mL | 0.1127 mL | 0.2255 mL | 0.4509 mL | 0.5636 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
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Crenolanib (CP-868596) is a potent, specific, and orally available inhibitor of PDGFRα, PDGFRβ and FLT3 with inhibitor-binding constant (Kd) of 3.2, 2.1, and 0.74 nM, respectively [1].
It has been shown that crenolanib is more potent than quizartinib and sorafenib at blocking FLT3 autophosphorylation and causing cytotoxicity [2]. Crenolanib is confirmed to be100-fold more potent than imatinib at suppressing D842V mutation. In addition, it has been reported that crenolanib inhibits PDGFRα D842V mutation rather than V561D mutation, with IC50 value of 10 nM [1]. In EOL-1 cells, crenolanib also inhibits the FIP1L1-PDGFRA fusion kinase activity (IC50=1 nM) and cell proliferation (IC50= 0.2 pM)[1].
References:
[1] Heinrich MC1, Griffith D, McKinley A, Patterson J, Presnell A, Ramachandran A, Debiec-Rychter M.
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] Galanis A1, Ma H, Rajkhowa T, Ramachandran A, Small D, Cortes J, Levis M. Crenolanib is a potent inhibitor of FLT3 with activity against resistance-conferring point mutants. Blood. 2014 Jan 2;123(1):94-100.- 3,4-Dihydroxy-2-methoxyxanthone
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