WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 573271
CAS#: 670220-93-6 (besylate)
Description: Crenolanib is a n orally bioavailable small molecule, targeting the platelet-derived growth factor receptor (PDGFR), with potential antineoplastic activity. Crenolanib binds to and inhibits PDGFR, which may result in the inhibition of PDGFR-related signal transduction pathways, and, so, the inhibition of tumor angiogenesis and tumor cell proliferation.
MedKoo Cat#: 573271
Name: Crenolanib besylate
CAS#: 670220-93-6 (besylate)
Chemical Formula: C32H35N5O5S
Exact Mass: 601.2359
Molecular Weight: 601.72
Elemental Analysis: C, 63.88; H, 5.86; N, 11.64; O, 13.29; S, 5.33
This product is not in stock, which may be available by custom synthesis.
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Related CAS #: 670220-93-6 (besylate) 670220-88-9 (free base)
Synonym: Crenolanib besylate; CP 868596; CP868596; CP-868596; ARO 002; RO-002; RO002; Crenolanib;
IUPAC/Chemical Name: 4-Piperidinamine, 1-(2-(5-((3-methyl-3-oxetanyl)methoxy)-1H-benzimidazol-1-yl)-8- quinolinyl)-, benzenesulfonate (1:1)
InChi Key: ARQUTWAXTHJROR-UHFFFAOYSA-N
InChi Code: 1S/C26H29N5O2.C6H6O3S/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;7-10(8,9)6-4-2-1-3-5-6/h2-8,13,17,19H,9-12,14-16,27H2,1H3;1-5H,(H,7,8,9)
SMILES Code: CC1(COc2ccc3c(c2)ncn3c4ccc5cccc(N6CCC(N)CC6)c5n4)COC1.OS(=O)(=O)c7ccccc7
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 601.72 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Melaiu O, Catalano C, De Santi C, Cipollini M, Figlioli G, Pellè L, Barone E, Evangelista M, Guazzelli A, Boldrini L, Sensi E, Bonotti A, Foddis R, Cristaudo A, Mutti L, Fontanini G, Gemignani F, Landi S. Inhibition of the platelet-derived growth factor receptor beta (PDGFRB) using gene silencing, crenolanib besylate, or imatinib mesylate hampers the malignant phenotype of mesothelioma cell lines. Genes Cancer. 2017 Jan;8(1-2):438-452. doi: 10.18632/genesandcancer.129. PubMed PMID: 28435517; PubMed Central PMCID: PMC5396622.
2: Hayashi Y, Bardsley MR, Toyomasu Y, Milosavljevic S, Gajdos GB, Choi KM, Reid-Lombardo KM, Kendrick ML, Bingener-Casey J, Tang CM, Sicklick JK, Gibbons SJ, Farrugia G, Taguchi T, Gupta A, Rubin BP, Fletcher JA, Ramachandran A, Ordog T. Platelet-Derived Growth Factor Receptor-α Regulates Proliferation of Gastrointestinal Stromal Tumor Cells With Mutations in KIT by Stabilizing ETV1. Gastroenterology. 2015 Aug;149(2):420-32.e16. doi: 10.1053/j.gastro.2015.04.006. Epub 2015 Apr 9. PubMed PMID: 25865047; PubMed Central PMCID: PMC4516576.
3: Mathias TJ, Natarajan K, Shukla S, Doshi KA, Singh ZN, Ambudkar SV, Baer MR. The FLT3 and PDGFR inhibitor crenolanib is a substrate of the multidrug resistance protein ABCB1 but does not inhibit transport function at pharmacologically relevant concentrations. Invest New Drugs. 2015 Apr;33(2):300-9. doi: 10.1007/s10637-015-0205-y. Epub 2015 Jan 20. PubMed PMID: 25597754.
