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Crenolanib (CP-868596) (670220-88-9)

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.

Not Intended for Therapeutic Use. For research use only.

CAS: 670220-88-9 Category

Crenolanib (CP-868596) (670220-88-9) Description:

Crenolanib is an orally bioavailable benzimidazole targeting the platelet-derived growth factor receptor (PDGFR) subtypes alpha and beta and FMS-related tyrosine kinase 3 (Flt3), with potential antineoplastic activity. Upon oral administration, crenolanib binds to and inhibits both wild-type and mutated forms of PDGFR and Flt3, which may result in the inhibition of PDGFR- and Flt3-related signal transduction pathways. This results in inhibition of tumor angiogenesis and tumor cell proliferation in PDGFR and/or Flt3 overexpressing tumor cells. PDGFR and Flt3, class III receptor tyrosine kinases, are upregulated or mutated in many tumor cell types.

Crenolanib (CP-868596) (670220-88-9) Specifications:

Product Name Crenolanib (CP-868596)
Synonyms CP-868596; ARO-002; UNII-LQF7I567TQ;CP 868596; CP868596; ARO 002; RO-002; RO002;
Chemical Name 1-[2-[5-[(3-methyloxetan-3-yl)methoxy]benzimidazol-1-yl]quinolin-8-yl]piperidin-4-amine
Purity >98%
CAS Number 670220-88-9
Molecular Formula C26H29N5O2
Molecular Weight 443.551 g/mol
Monoisotopic Mass 443.232 g/mol
MDL number MFCD21609260
InChIKey DYNHJHQFHQTFTP-UHFFFAOYSA-N
InChi Code 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
SMILES CC1(COC1)COC2=CC3=C(C=C2)N(C=N3)C4=NC5=C(C=CC=C5N6CCC(CC6)N)C=C4
Form powder
Color Off-white
Solubility  Soluble in DMSO
Storage Temp.  0 – 4 C for short term (days to weeks), or -20 C for long term (months).
Shelf life >2 years if stored properly
Handling Protect from air and light
Application PDGFR Inhibitor

 


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RIDADR NONH for all modes of transport

References:

  1. Clinical resistance to crenolanib in acute myeloid leukemia due to diverse molecular mechanisms. Zhang H, Savage S, Schultz AR, Bottomly D, White L, Segerdell E, Wilmot B, McWeeney SK, Eide CA, Nechiporuk T, Carlos A, Henson R, Lin C, Searles R, Ho H, Lam YL, Sweat R, Follit C, Jain V, Lind E, Borthakur G, Garcia-Manero G, Ravandi F, Kantarjian HM, Cortes J, Collins R, Buelow DR, Baker SD, Druker BJ, Tyner JW. Nat Commun. 2019 Jan 16;10(1):244. doi: 10.1038/s41467-018-08263-x.
  2. CAR T-cells targeting FLT3 have potent activity against FLT3-ITD+ AML and act synergistically with the FLT3-inhibitor crenolanib. Jetani H, Garcia-Cadenas I, Nerreter T, Thomas S, Rydzek J, Meijide JB, Bonig H, Herr W, Sierra J, Einsele H, Hudecek M. Leukemia. 2018 May;32(5):1168-1179. doi: 10.1038/s41375-018-0009-0. Epub 2018 Feb 5.
  3. Azacitidine combined with the selective FLT3 kinase inhibitor crenolanib disrupts stromal protection and inhibits expansion of residual leukemia-initiating cells in FLT3-ITD AML with concurrent epigenetic mutations.
  4. Garz AK, Wolf S, Grath S, Gaidzik V, Habringer S, Vick B, Rudelius M, Ziegenhain C, Herold S, Weickert MT, Smets M, Peschel C, Oostendorp RAJ, Bultmann S, Jeremias I, Thiede C, Döhner K, Keller U, Götze KS. Oncotarget. 2017 Oct 16;8(65):108738-108759. doi: 10.18632/oncotarget.21877. eCollection 2017 Dec 12.
  5. Crenolanib is a type I tyrosine kinase inhibitor that inhibits mutant KIT D816 isoforms prevalent in systemic mastocytosis and core binding factor leukemia. Kampa-Schittenhelm KM, Frey J, Haeusser LA, Illing B, Pavlovsky AA, Blumenstock G, Schittenhelm MM. Oncotarget. 2017 Aug 7;8(47):82897-82909. doi: 10.18632/oncotarget.19970. eCollection 2017 Oct 10.
  6. Effects of crenolanib, a nonselective inhibitor of PDGFR, in a mouse model of transient middle cerebral artery occlusion. Wang J, Fu X, Zhang D, Yu L, Lu Z, Gao Y, Liu X, Man J, Li S, Li N, Wang M, Liu X, Chen X, Zang W, Yang Q, Wang J.Neuroscience. 2017 Nov 19;364:202-211. doi: 10.1016/j.neuroscience.2017.09.025. Epub 2017 Sep 21.
  7. 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. 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. Genes Cancer. 2017 Jan;8(1-2):438-452. doi: 10.18632/genesandcancer.129.