[CAS NO. 899805-25-5] Tanzisertib(CC-930)
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PRODUCTS SPECIFICATIONS [899805-25-5]
Store
Catalog
SLK-S8490
Brand
Selleck
CAS
899805-25-5
DESCRIPTION [899805-25-5]
Overview
| MDL | MFCD23160040 |
|---|---|
| Molecular Weight | 484.9 |
| Molecular Formula | C21H23F3N6O2.HCl |
| SMILES | O[C@H]1CC[C@H](NC2=NC=C3N=C(NC4=C(F)C=C(F)C=C4F)N([C@@H]5COCC5)C3=N2)CC1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0623 mL | 10.3114 mL | 20.6228 mL |
| 5 mM | 0.4125 mL | 2.0623 mL | 4.1246 mL |
| 10 mM | 0.2062 mL | 1.0311 mL | 2.0623 mL |
| 50 mM | 0.0412 mL | 0.2062 mL | 0.4125 mL |
Description
Tanzisertib (CC-930, JNK-930, JNKI-1) is kinetically competitive with ATP in the -dependent phosphorylation of the protein substrate c-Jun and potent against all isoforms of (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
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.
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