≥99% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at 2-8°C,Desiccated Ships Wet ice 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.
SCH-1473759 hydrochloride is an aurora inhibitor with IC 50 s of 4 and 13 nM for aurora A and B, respectively.
In Vitro
SCH-1473759 directly binds to aurora A and B with K d s of 20 and 30 nM, respectively. SCH-1473759 also inhibits the Src family of kinases (IC 50 <10 nM), Chk1 (IC 50 =13 nM), VEGFR2 (IC 50 =1 nM), and IRAK4 (IC 50 =37 nM). It does not have significant activity (IC 50 >1000 nM) against 34 other kinases representing different families of the kinome. SCH-1473759 inhibits HCT116 cells proliferation with an IC 50 of 6 nM. SCH 1473759 inhibits tumor cell lines from different tissues (breast, ovarian, prostate, lung, colon, brain, gastric, renal, skin, and leukemia). The most sensitive cell lines includ A2780, LNCap, N87, Molt4, K562, and CCRF-CEM with IC 50 values <5 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SCH-1473759 at a low dose of 5 mg/kg (ip, bid) is well-tolerated in a continuous dosing schedule and shows 50% tumor growth inhibition(TGI) on day 16. A higher dose of 10mg/kg(ip, bid) is well-tolerated in an intermittent schedule (5 days on, 5 days off) and gave 69% TGI on day 16. SCH-1473759 shows good exposure in all species with the clearance being high in rodents and moderate in dog and monkey. The half-life is also moderate, but the tissue distribution is high . SCH 1473759 dose- and schedule-dependent anti-tumor activity in four human tumor xenograft models. Further, the efficacy is enhanced in combination with taxanes and found to be most efficacious when SCH 1473759 is dosed 12-h post-taxane treatment. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal administration
Mice: Anti-tumor efficacy of SCH 1473759 dosed i.p. is evaluated in mice bearing established A2780 ovarian tumor xenografts. Three schedules are tested at their respective maximum tolerated doses: 10 mg/kg bid (twice daily), 20 mg/kg qd (daily), and 100 mg/kg day 0, 4, 7. Additionally, 60 mg/kg day 0, 4, 7 is tested . aladdin has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:Aurora A 4 nM (IC 50 ) Aurora B 13 nM (IC 50 )
| Canonical Smiles | CCN(CC1=NSC(=C1)NC2=NC(=CN3C2=NC=C3C4=CNN=C4)C)C(C)(C)CO.Cl |
|---|---|
| IUPAC Name | 2-[ethyl-[[5-[[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]amino]-1,2-thiazol-3-yl]methyl]amino]-2-methylpropan-1-ol;hydrochloride |
| InChIKey | YBAZMWNWFHDNTH-UHFFFAOYSA-N |
| INCHI | 1S/C20H26N8OS.ClH/c1-5-27(20(3,4)12-29)11-15-6-17(30-26-15)25-18-19-21-9-16(14-7-22-23-8-14)28(19)10-13(2)24-18;/h6-10,29H,5,11-12H2,1-4H3,(H,22,23)(H,24,25);1H |
| Isomeric SMILES | CCN(CC1=NSC(=C1)NC2=NC(=CN3C2=NC=C3C4=CNN=C4)C)C(C)(C)CO.Cl |
| PubChem CID | 53317913 |
| Molecular Weight | 463.00 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
Download SDS →Lot-specific quality data. Enter your lot number to retrieve the exact COA.
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View spec sheet →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| Class | Imidazopyrazines |
| Subclass | Not available |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Imidazopyrazines |
| Alternative Parents | Aralkylamines Aminopyrazines N-substituted imidazoles Imidolactams Aminothiazoles Pyrazoles Heteroaromatic compounds Trialkylamines 1,2-aminoalcohols Azacyclic compounds Primary alcohols Hydrochlorides Hydrocarbon derivatives |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | Imidazopyrazine - Aminopyrazine - Aralkylamine - 1,2-thiazolamine - N-substituted imidazole - Pyrazine - Imidolactam - Azole - Imidazole - Heteroaromatic compound - Pyrazole - Thiazole - 1,2-aminoalcohol - Tertiary amine - Tertiary aliphatic amine - Azacycle - Organic nitrogen compound - Amine - Primary alcohol - Organooxygen compound - Organonitrogen compound - Hydrocarbon derivative - Alcohol - Organic oxygen compound - Hydrochloride - Aromatic heteropolycyclic compound |
| Description | This compound belongs to the class of organic compounds known as imidazopyrazines. These are organic heteropolycyclic compounds containing a pyrazine ring fused to an imidazole ring. These also include hydrogenated derivatives of the imidazopyrazine moiety. Imidazole is 5-membered ring consisting of three carbon atoms, and two nitrogen centers at the 1- and 3-positions. Pyrazine is a 6-membered ring consisting of six carbon atoms and two nitrogen centers at ring positions 1 and 4. |
| External Descriptors | Not available |
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| Solubility | H2O : 8.33 mg/mL (17.99 mM; ultrasonic and warming and heat to 60°C) DMSO : 7.14 mg/mL (15.42 mM; ultrasonic and warming and heat to 60°C) |
|---|---|
| Molecular Weight | 463.000 g/mol |
| XLogP3 | |
| Hydrogen Bond Donor Count | 4 |
| Hydrogen Bond Acceptor Count | 8 |
| Rotatable Bond Count | 8 |
| Exact Mass | 462.172 Da |
| Monoisotopic Mass | 462.172 Da |
| Topological Polar Surface Area | 136.000 Ų |
| Heavy Atom Count | 31 |
| Formal Charge | 0 |
| Complexity | 569.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 2 |
