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Datasheet of CC-930

Description:.
CC-930(Tanzisertib) is a selective and potent JNK1/JNK2/JNK3(IC50=61/7/6 nM) inhibitor and is currently under clinical
development for fibrotic and infammatory indications.
in vitro: Compound 1 (CC-930) showed remarkable selectivity in a panel of 240 kinases, EGFR being the only non-MAP kinase
inhibited more than 50% at 3 lM (IC50 = 0.38 lM). It inhibited no receptor at greater than 50% at 10 lM concentration in a panel
of 75 receptors, ion channels and neurotransmitter transporters. Finally, when tested against 22 diverse non-kinase enzymes at 10
lM, no inhibition greater than 50% was observed. Incubation with CC-930 prevented the phosphorylation of c-Jun and reduced
the stimulatory levels of these cytokines on the release of collagen.
in vivo: Inhibition of JNK by CC-930 prevented dermal thickening, myofibroblast differentiation and the accumulation of
collagen in a dose-dependent manner in mice challenged with bleomycin and in TSK1 mice. In addition to the prevention of
fibrosis, treatment with pharmacologically relevant doses of CC-930 also induced regression of established experimental
fibrosis. CC-930 did not affect blood pressure, kidney hypertrophy, glomerular hyperfiltration, podocyte loss, glomerular
fibrosis or tubulointerstitial injury in diabetic SHR (spontaneously hypertensive rats). However, CC-930 reduced macrophages
and ccl2 mRNA levels in diabetic kidneys.
Toxicity: There were no deaths or AEs that led to withdrawal during the study. Fifteen (33%) subjects reported a total of 22
treatment-emergent adverse events (TEAEs). Subject 207 (25-mg CC-930 group) was involved in a road traffic accident 6 days
after the dose and was hospitalized. This adverse event was considered as a serious adverse event but not related to the study
drug. The severity of all other adverse events was rated as mild..

Chemical Information
Catalog

DC7311

Purity of current batch:

>98%

Molecular Weight (MW)

448.44153

Molecular Formula

C21H23F3N6O2

CAS No.

899805-25-5

Solubility (25C)

DMSO

Storage

Store at -20C (desiccating conditions).

Handling:
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in
advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable
for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room
temperature for at least 1 hour.