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Tanzisertib(CC-930) - 99%, high purity , CAS No.899805-25-5(freebase)

COA

Grade & Purity:

Moligand™

≥99%

Cas Number: 899805-25-5(freebase)
Molecular Weight: 484.9

In stock

Item Number

T414026

Grouped product items
SKU	Size	Availability	Price	Qty
T414026-5mg	5mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$393.90
T414026-25mg	25mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$1,328.90

JNK Inhibitors

Basic Description

Synonyms	JNK-930 \| JNKI-1trans- 4-[[9-[(3S)-tetrahydro-3-furanyl]-8-[(2,4,6-trifluorophenyl)amino]-9H-purin-2-yl]amino]-Cyclohexanol hydrochloride
Specifications & Purity	Moligand™, ≥99%
Biochemical and Physiological Mechanisms	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 Temp	Store at -20°C
Shipped In	Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available.
Grade	Moligand™
Product Description	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

Associated Targets(Human)

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)

Names and Identifiers

Smiles	Cl.OC1CCC(CC1)NC2=NC3=C(C=N2)N=C(NC4=C(F)C=C(F)C=C4F)[N]3C5CCOC5
Molecular Weight	484.9

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

Chemical and Physical Properties

Solubility	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);

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