Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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C127776-5mg | 5mg | In stock | $98.90 | |
C127776-10mg | 10mg | In stock | $157.90 | |
C127776-25mg | 25mg | In stock | $247.90 | |
C127776-50mg | 50mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $336.90 | |
C127776-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $554.90 |
Potent PDGFR and FLT3 inhibitor
Synonyms | Crenolanib | 670220-88-9 | Crenolanib (CP-868596) | CP-868596 | ARO-002 | Crenolanib [USAN] | CP-868,596 | ARO 002 | CP 868596 | CP-868596 (Crenolanib) | 1-(2-(5-((3-Methyloxetan-3-yl)methoxy)-1H-benzo-[d]imidazol-1-yl)quinolin-8-yl)piperidin-4-amine | LQF7I567TQ | CP868569 | Cren |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Potent inhibitor of PDGFR (Kd for alpha = 2.1 nM; beta = 3.2 nM) and FLT3 (Kd = 0.74 nM). Type I inhibitor that binds only the active kinase conformation. Active towards imatinib-resistance assciated PDGFR-alpha mutations (D842I, D842V, D842Y, DI842-843M |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Tyrosine-protein kinase receptor FLT3 inhibitor |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Refer to SDS for further information Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | Crenolanib (CP-868596, ARO 002) is a potent and selective PDGFRα/β inhibitor with a Kd of 2.1 nM/3.2 nM in CHO cells. It can also effectively inhibit FLT3. It is sensitive to the D842V mutant and sensitive to the V561D mutant. It is not sensitive, and the selectivity for PDGFR is more than 100 times higher than that for c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB2, and Src. Crenolanib can help induce mitochondrial autophagy. |
ALogP | 3.7 |
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IUPAC Name | 1-[2-[5-[(3-methyloxetan-3-yl)methoxy]benzimidazol-1-yl]quinolin-8-yl]piperidin-4-amine |
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INCHI | 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 |
InChi Key | DYNHJHQFHQTFTP-UHFFFAOYSA-N |
Canonical SMILES | CC1(COC1)COC2=CC3=C(C=C2)N(C=N3)C4=NC5=C(C=CC=C5N6CCC(CC6)N)C=C4 |
Isomeric SMILES | CC1(COC1)COC2=CC3=C(C=C2)N(C=N3)C4=NC5=C(C=CC=C5N6CCC(CC6)N)C=C4 |
PubChem CID | 10366136 |
Molecular Weight | 443.54 |
PubChem CID | 10366136 |
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CAS Registry No. | 670220-88-9 |
ChEMBL Ligand | CHEMBL2105728 |
Wikipedia | Crenolanib |
RCSB PDB Ligand | 6T2 |
Reactome Reaction | R-HSA-9702583, R-HSA-9702508, R-HSA-9695828, R-HSA-9674427, R-HSA-9674093 |
Reactome Drug | R-ALL-9674072 |
Enter Lot Number to search for COA:
To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section
Lot Number | Certificate Type | Date | Item |
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B2207046 | Certificate of Analysis | Nov 13, 2023 | C127776 |
B2207047 | Certificate of Analysis | Nov 13, 2023 | C127776 |
B2207048 | Certificate of Analysis | Nov 13, 2023 | C127776 |
B2207306 | Certificate of Analysis | Nov 13, 2023 | C127776 |
B2207307 | Certificate of Analysis | Jan 04, 2022 | C127776 |
Solubility | ≥22.2mg/mL in DMSO, ≥2.5 mg/mL in EtOH with ultrasonic,insoluble in H2O |
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1. Heinrich MC, Griffith D, McKinley A, Patterson J, Presnell A, Ramachandran A, Debiec-Rychter M. (2012) Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors.. Clin Cancer Res, 18 (16): (4375-84). [PMID:22745105] |
2. Zimmerman EI, Turner DC, Buaboonnam J, Hu S, Orwick S, Roberts MS, Janke LJ, Ramachandran A, Stewart CF, Inaba H et al.. (2013) Crenolanib is active against models of drug-resistant FLT3-ITD-positive acute myeloid leukemia.. Blood, 122 (22): (3607-15). [PMID:24046014] |
3. Smith CC, Lasater EA, Lin KC, Wang Q, McCreery MQ, Stewart WK, Damon LE, Perl AE, Jeschke GR, Sugita M et al.. (2014) Crenolanib is a selective type I pan-FLT3 inhibitor.. Proc Natl Acad Sci USA, 111 (14): (5319-24). [PMID:24623852] |