Tanzisertib(CC-930) - Moligand™, ≥99% , CAS No.899805-25-5(freebase)

CAS: 899805-25-5(freebase) Cat. No.: T414026 Summenformel: C₂₁H₂₃F₃N₆O₂.HCl Molekulargewicht: 484.9

GRADE & PURITY Moligand™, ≥99%

Synonyms

JNK-930 | JNKI-1trans- 4-​[[9-​[(3S)​-​tetrahydro-​3-​furanyl]​-​8-​[(2,​4,​6-​trifluorophenyl)​amino]​-​9H-​purin-​2-​yl]​amino]​-​Cyclohexanol hydrochloride

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Übersicht

Information

Tanzisertib(CC-930) Tanzisertib (CC-930, JNK-930, JNKI-1) is kinetically competitive with ATP in the JNK -dependent phosphorylation of the protein substrate c-Jun and potent against all isoforms of JNK (Ki(JNK1) = 44 ± 3 nM, IC50(JNK1) = 61 nM, Ki(JNK2) = 6.2 ± 0.6 nM, IC50(JNK2) = 5 nM, IC50(JNK3) = 5 nM) and selective against MAP kinases ERK1 and p38a with IC50 of 0.48 and 3.4 μM respectively.

Targets

JNK3 (Cell-free assay); JNK2 (Cell-free assay); JNK1 (Cell-free assay) 0.006 μM; 0.007 μM; 0.061 μM

In vitro

CC-930 inhibits the formation of phospho-cJun in human PBMC stimulated by phorbol-12-myristate-13-acetate and phytohemeagglutinin (IC50 = 1 μM). CC-930 shows remarkable selectivity in a panel of 240 kinases, EGFR being the only non-MAP kinase inhibited more than 50% at 3 μM (IC50 = 0.38 μM). It inhibits no receptor at greater than 50% at 10 μM concentration in a panel of 75 receptors, ion channels and neurotransmitter transporters. CC-930 does not inhibit CYP P450 enzymes significantly and is metabolized by CYP 3A4 and 2D6.

In vivo

In the acute rat LPS-induced TNFα production PK-PD model, the compound inhibits the production of TNFα by 23% and 77% at 10 and 30 mg/kg oral dose respectively. CC-930 is well-tolerated and exposure is dose-proportional.

Cell Research(from reference)

Cell lines：Jurkat T cells 

Incubation Time：30 minutes 

Specifications

Synonyme

JNK-930 | JNKI-1trans- 4-​[[9-​[(3S)​-​tetrahydro-​3-​furanyl]​-​8-​[(2,​4,​6-​trifluorophenyl)​amino]​-​9H-​purin-​2-​yl]​amino]​-​Cyclohexanol hydrochloride

Spezifikationen & Reinheit

Moligand™, ≥99%

Biochemische und physiologische Mechanismen

Tanzisertib (CC-930, JNK-930, JNKI-1) is kinetically competitive with ATP in the JNK-dependent phosphorylation of the protein substrate c-Jun and potent against all isoforms of JNK (Ki(JNK1) = 44 ± 3 nM, IC50(JNK1) = 61 nM, Ki(JNK2) = 6.2 ± 0.6 nM, IC50(J

Storage

Store at -20°C

Verschickt in

Ice chest + Ice pads

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Note

Moligand™

Reinheit

≥99%

Namen und Kennungen

Kanonisches Lächeln

Cl.OC1CCC(CC1)NC2=NC3=C(C=N2)N=C(NC4=C(F)C=C(F)C=C4F)[N]3C5CCOC5

Molekulargewicht

484.9

Zugehörige Ziele (menschlich)

MAPK10 Tchem Mitogen-activated protein kinase 10 (4 Activities)

Discover Target: MAPK10

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAPK8 Tchem Mitogen-activated protein kinase 8 (2 Activities)

Discover Target: MAPK8

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAPK9 Tchem Mitogen-activated protein kinase 9 (6 Activities)

Discover Target: MAPK9

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemische und physikalische Eigenschaften

• Löslichkeit: Solubility (25°C) In vitro DMSO: 89 mg/mL warmed with 50ºC Water: bath (183.54 mM); Ethanol: 89 mg/mL warmed with 50ºC Water: bath (183.54 mM); Water: 4 mg/mL warmed with 50ºC Water: bath (8.24 mM)