10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Information
CX-6258 HCl is a potent, orally efficacious pan-Pim kinaseinhibitor withIC50of 5 nM, 25 nM and 16 nM for Pim1, Pim2, and Pim3, respectively.
Targets
Pim1 (Cell-free assay); Pim3 (Cell-free assay); Pim2 (Cell-free assay) 5 nM; 16 nM; 25 nM
In vitro
CX-6258 shows antiproliferative activity against a panel of human cancer cell lines with IC50 of 0.02-3.7 μM, mostly sensitive to acute leukemia cell lines. Combinations of CX-6258 with doxorubicin (10:1 molar ratio) and CX-6258 with paclitaxel (100:1 molar ratio) produces synergistic cell killing with combination index (CI50) values equal to 0.4 and 0.56, respectively. CX-6258 causes dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively.
In vivo
CX-6258 exhibits dose dependent efficacy in suppressing tumor growth in mice carrying MV-4-11 xenografts, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGI
Cell Research(from reference)
Cell lines：ALL, AML, CML, PML and MM cell lines
Concentrations：~10 μM
Incubation Time：96 hours
| ALogP | 4.416 |
|---|---|
| hba_count | 3 |
| Recuento HBD | 1 |
| Enlace rotable | 3 |
| Sonrisas canónicas | CN1CCCN(CC1)C(=O)C2=CC=CC(=C2)C3=CC=C(O3)C=C4C5=C(C=CC(=C5)Cl)NC4=O.Cl |
|---|---|
| IUPAC Name | (3E)-5-chloro-3-[[5-[3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl]furan-2-yl]methylidene]-1H-indol-2-one;hydrochloride |
| InChIKey | YYIMMVXTWBIEAG-YHLMHSEJSA-N |
| INCHI | 1S/C26H24ClN3O3.ClH/c1-29-10-3-11-30(13-12-29)26(32)18-5-2-4-17(14-18)24-9-7-20(33-24)16-22-21-15-19(27)6-8-23(21)28-25(22)31;/h2,4-9,14-16H,3,10-13H2,1H3,(H,28,31);1H/b22-16+; |
| Isómeros SMILES | CN1CCCN(CC1)C(=O)C2=CC=CC(=C2)C3=CC=C(O3)/C=C/4\C5=C(C=CC(=C5)Cl)NC4=O.Cl |
| Peso molecular | 498.4 |
| Reaxy-Rn | 36132332 |
| Reaxys-RN_link_address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=36132332&ln= |
Comprehensive hazard, handling, storage, and regulatory compliance document.
Download SDS →Lot-specific quality data. Enter your lot number to retrieve the exact COA.
Look up COA →Full quality attributes and acceptance criteria for this grade.
View spec sheet →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| Clase | Indoles and derivatives |
| Subclass | Indolines |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Indolines |
| Alternative Parents | Benzamides Benzoyl derivatives 1,4-diazepanes Aryl chlorides Tertiary carboxylic acid amides Heteroaromatic compounds Furans Trialkylamines Secondary carboxylic acid amides Amino acids and derivatives Lactams Oxacyclic compounds Azacyclic compounds Carbonyl compounds Hydrocarbon derivatives Hydrochlorides Organic oxides Organochlorides |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | Benzamide - Benzoic acid or derivatives - Dihydroindole - Benzoyl - 1,4-diazepane - Diazepane - Aryl chloride - Aryl halide - Monocyclic benzene moiety - Benzenoid - Tertiary carboxylic acid amide - Furan - Heteroaromatic compound - Tertiary amine - Secondary carboxylic acid amide - Tertiary aliphatic amine - Amino acid or derivatives - Carboxamide group - Lactam - Azacycle - Oxacycle - Carboxylic acid derivative - Organooxygen compound - Organohalogen compound - Carbonyl group - Hydrocarbon derivative - Organic oxide - Organochloride - Organic oxygen compound - Amine - Organic nitrogen compound - Organonitrogen compound - Hydrochloride - Aromatic heteropolycyclic compound |
| Descripción | This compound belongs to the class of organic compounds known as indolines. These are compounds containing an indole moiety, which consists of pyrrolidine ring fused to benzene to form 2,3-dihydroindole. |
| External Descriptors | Not available |
| DMSO (mg/ml) Solubilidad máxima | 57 |
|---|---|
| DMSO (mM) Solubilidad máxima | 114.3659711 |
| Agua (mg/ml) Solubilidad máxima | 89 |
| Agua (mM) Solubilidad máxima | 178.5714286 |
| Peso molecular | 498.400 g/mol |
| XLogP3 | |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 4 |
| Rotatable Bond Count | 3 |
| Exact Mass | 497.127 Da |
| Monoisotopic Mass | 497.127 Da |
| Topological Polar Surface Area | 65.800 Ų |
| Heavy Atom Count | 34 |
| Formal Charge | 0 |
| Complexity | 774.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 1 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 1 |
| Covalently-Bonded Unit Count | 2 |
