| Identification | Back Directory | [Name]
Crenolanib | [CAS]
670220-88-9 | [Synonyms]
ARO 002
CP868569
CP 868596
Crenolanib
Crenolanib, >=98%
CP868569/Crenolanib
cp-868596 crenolanib
Crenolanib (CP-868569)
Crenolanib (CP-868596)
[1-[2-[5-(3-Methyloxetan-3-ylMethoxy)benziMidazol-1-yl]quinolin-8-yl]piperidin-4-yl]aMine
1-[2-[5-[(3-Methyl-3-oxetanyl)Methoxy]-1H-benziMidazol-1-yl]-8-quinolinyl]-4-piperidinaMine
1-(2-(5-((3-Methyloxetan-3-yl)methoxy)-1H-benzo-[d]imidazol-1-yl)quinolin-8-yl)piperidin-4-ami
1-(2-(5-((3-methyloxetan-3-yl)methoxy)-1H-benzo[d]imidazol-1-yl)quinolin-8-yl)piperidin-4-amine
[1-[2-[5-(3-Methyloxetan-3-ylmethoxy)benzimidazol-1-yl]quinolin-8-yl]piperidin-4-yl]amine Crenolanib ,ARO 002 | [Molecular Formula]
C26H29N5O2 | [MDL Number]
MFCD21609260 | [MOL File]
670220-88-9.mol | [Molecular Weight]
443.541 |
| Chemical Properties | Back Directory | [Boiling point ]
676.6±65.0 °C(Predicted) | [density ]
1.36 | [storage temp. ]
-20° | [solubility ]
Soluble in DMSO (up to 15 mg/ml) or in Ethanol (up to 10 mg/ml). | [form ]
solid | [pka]
9.84±0.20(Predicted) | [color ]
White | [Stability:]
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month. | [CAS DataBase Reference]
670220-88-9 |
| Hazard Information | Back Directory | [Uses]
Crenolanib (CP-868569) is a highly selective and potent PDGFR-α inhibitor with IC50 of 0.9 and 1.8 nM against PDGFRα and PDGFRβ, respectively. | [Uses]
Crenolanib (CP-868569) is a tyrosine kinase inhibitor that acts by specifically inhibiting the receptor tyrosine kinases PDGFRα and PDGFRβ. Crenolanib (CP-868569) inhibits the activity of PDGFRα D842V kinase and prevented the phosphorylation of wild type PDGFRα. Crenolanib (CP-868569) possesses potential antineoplastic activity. Crenolanib is believed to suppress PDGFR-related signal transduction pathways leading to the inhibition of tumor angiogenesis and tumor cell proliferation. | [Uses]
Crenolanib is an orally bioavailable, selective inhibitor of type III tyrosine kinases with nanomolar potencies against platelet-derived growth factor receptor α (PDGFRα) and PDGFRβ and Fms-related tyrosine kinase 3 (FLT3; IC50s = 11, 3.2, and 4 nM, respectively). It also inhibits medically-relevant mutant forms of these kinases, including the D842V-containing form of PDGFR and D835Y and internal tandem duplication mutations of FLT3, at nanomolar concentrations. Crenolanib is more than 100-fold selective for these kinases over other tyrosine and serine/threonine kinases. It is effective when used in cells and in vivo.[Cayman Chemical] | [Description]
Crenolanib (670220-88-9) is a potent inhibitor of PDGFR (Kd?for α = 2.1 nM; β = 3.2 nM) and FLT3 (Kd?= 0.74 nM).1?Crenolanib is a type I inhibitor binding only to the active kinase conformation. It showed potent activity against imatinib-resistant PDGFRα mutations D842I, D842V, D842Y, DI842-843M, and deletion I8432?as well as FLT3/ITD and FLT3/D835 mutants3. Crenolanib acted synergistically with FLT3-CAR T-cells in a FLT3-ITD+?AML murine xenograft model.4 | [Definition]
ChEBI:Crenolanib is a member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a 8-(4-aminopiperidin-1-yl)quinolin-2-yl group at position 1 and by a (3-methyloxetan-3-yl)methoxy group at position 5. It is an inhibitor of type III tyrosine kinases, PDGFRalpha/beta and FLT3 (IC50 of 11, 3.2, and 4 nM). Currently under clinical development for the treatment of acute myeloid leukemia. It has a role as an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, an angiogenesis inhibitor, an antineoplastic agent and an apoptosis inducer. It is a member of benzimidazoles, an aromatic ether, a member of quinolines, a member of oxetanes, an aminopiperidine and a tertiary amino compound. | [target]
PDGFRα | [storage]
Store at -20°C | [References]
1) Lewis?et al.?(2009)?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.?27?5262
2) Smith?et al.?(2014)?Crenolanib is a selective type I pan-FLT3 inhibitor; Proc. Natl. Acad. Sci. USA?111?5319
3) Heinrich?et al.?(2012)?Crenolanib Inhibits Drug-Resistant PDGFRA D842V Mutation Associated with Imatinib-Resistant Gastrointestinal Stromal Tumors; Clin. Cancer Res.?18?4375
4) Jetani?et al.?(2018)?CAR T-cells targeting FLT3 have potent activity against FLT-ITD+ AML and act synergistically with the FLT3-inhibitor crenolanib; Leukemia?32?1168 |
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