MedKoo Cat#: 573271 | Name: Crenolanib besylate

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

Crenolanib besylate
Crenolanib besylate
CAS#670220-93-6 (besylate)

Theoretical Analysis

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

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Synonym
Crenolanib besylate; Crenolanib besilate; CP 868596-26; CP868596-26; CP-868596-26; ARO 002-26; ARO-002-26; ARO002-26; 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
More Info

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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.