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
- Molecular Weight:
- 443.54
- MDL Number:
- MFCD21609260
- MOL File:
- 670220-88-9.mol
| 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 |
| FDA UNII | LQF7I567TQ |
| NCI Drug Dictionary | crenolanib |
Crenolanib price More Price(28)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 18873 | Crenolanib ≥95% | 670220-88-9 | 1mg | $47 | 2024-03-01 | Buy |
| Cayman Chemical | 18873 | Crenolanib ≥95% | 670220-88-9 | 5mg | $104 | 2024-03-01 | Buy |
| Cayman Chemical | 18873 | Crenolanib ≥95% | 670220-88-9 | 10mg | $182 | 2024-03-01 | Buy |
| Cayman Chemical | 18873 | Crenolanib ≥95% | 670220-88-9 | 50mg | $564 | 2024-03-01 | Buy |
| Usbiological | 007102 | Crenolanib | 670220-88-9 | 5mg | $496 | 2021-12-16 | Buy |
Crenolanib Chemical Properties,Uses,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 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]
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 (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.
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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| career henan chemical co | +86-0371-86658258 | sales@coreychem.com | China | 29914 | 58 |
| Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 967 | 58 |
| Hubei xin bonus chemical co. LTD | 86-13657291602 | linda@hubeijusheng.com | CHINA | 22968 | 58 |
| Chongqing Chemdad Co., Ltd | +86-023-61398051 +8613650506873 | sales@chemdad.com | China | 39916 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 29220 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| ZHEJIANG JIUZHOU CHEM CO., LTD | +86-0576225566889 +86-13454675544 | admin@jiuzhou-chem.com；jamie@jiuzhou-chem.com；alice@jiuzhou-chem.com | China | 20000 | 58 |
| Zhengzhou Anbu Chem Co.,Ltd | +86-0371-88006763; +8615988602810 | sales@anbuchem.com | China | 3000 | 58 |
View Lastest Price from Crenolanib manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2019-07-06 | Crenolanib
670220-88-9
|
US $7.00 / KG | 1KG | 99% | 100KG | Career Henan Chemical Co |
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- Crenolanib
670220-88-9
- US $7.00 / KG
- 99%
- Career Henan Chemical Co