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Crenolanib

Product Name
Crenolanib
CAS No.
670220-88-9
Chemical Name
Crenolanib
Synonyms
596;CS-72;CP-868;RO 002;ARO 002;CP868569;CP 868596;Crenolanib;Crenolanib, >=98%;CP868569/Crenolanib
CBNumber
CB02582957
Molecular Formula
C26H29N5O2
Formula Weight
443.54
MOL File
670220-88-9.mol
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Crenolanib Property

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
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical
Product number
18873
Product name
Crenolanib
Purity
≥95%
Packaging
1mg
Price
$47
Updated
2024/03/01
Cayman Chemical
Product number
18873
Product name
Crenolanib
Purity
≥95%
Packaging
5mg
Price
$104
Updated
2024/03/01
Cayman Chemical
Product number
18873
Product name
Crenolanib
Purity
≥95%
Packaging
10mg
Price
$182
Updated
2024/03/01
Cayman Chemical
Product number
18873
Product name
Crenolanib
Purity
≥95%
Packaging
50mg
Price
$564
Updated
2024/03/01
Usbiological
Product number
007102
Product name
Crenolanib
Packaging
5mg
Price
$496
Updated
2021/12/16
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Crenolanib Chemical Properties,Usage,Production

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

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]

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

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

Crenolanib Preparation Products And Raw materials

Raw materials

Preparation Products

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Crenolanib Suppliers

Novachemistry
Tel
44-20819178-90 02081917890
Fax
(0)2080432064
Email
info@novachemistry.com
Country
United Kingdom
ProdList
4381
Advantage
58
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View Lastest Price from Crenolanib manufacturers

Career Henan Chemical Co
Product
Crenolanib 670220-88-9
Price
US $7.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
100KG
Release date
2018-08-20

670220-88-9, CrenolanibRelated Search:


  • Crenolanib, >=98%
  • Crenolanib
  • [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
  • ARO 002
  • CP 868596
  • Crenolanib (CP-868569)
  • Crenolanib (CP-868596)
  • CP868569/Crenolanib
  • cp-868596 crenolanib
  • 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
  • 1-[2-[5-[(3-Methyl-3-oxetanyl)methoxy]-1-benzimidazolyl]-8-quinolyl]-4-piperidinamine
  • CS-72
  • 596
  • CP-868
  • CP-868;596; CP-868596; ARO 002;CP868596
  • 1-(2-(5-((3-Methyloxetan-3-yl)methoxy)-1H-benzo-[d]imidazol-1-yl)quinolin-8-yl)piperidin-4-ami
  • CP868569
  • CRENOLANIB;CP-868596;CP 868596;ARO 002
  • 4-Piperidinamine, 1-[2-[5-[(3-methyl-3-oxetanyl)methoxy]-1H-benzimidazol-1-yl]-8-quinolinyl]-
  • Crenolanib USP/EP/BP
  • RO 002
  • 670220-88-9
  • Inhibitors
  • Aromatics
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Tyrosine Kinase Inhibitors