[CAS NO. 1095382-05-0] CCT137690

Name: CCT137690
Brand: Arctom Scientific
SKU: SLK-S2744

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PRODUCTS SPECIFICATIONS [1095382-05-0]

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Catalog

SLK-S2744

Brand

Selleck

CAS

1095382-05-0

DESCRIPTION [1095382-05-0]

Overview

MDL	MFCD18206879
Molecular Weight	551.48
Molecular Formula	C26H31BrN8O
SMILES	CC1=CC(CN2CCN(C3=C4C(NC(C5=CC=C(N6CCN(C)CC6)C=C5)=N4)=NC=C3Br)CC2)=NO1

For research use only.

Storage

3 years,-20°C,powder
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

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.8133 mL	9.0665 mL	18.1330 mL
5 mM	0.3627 mL	1.8133 mL	3.6266 mL
10 mM	0.1813 mL	0.9067 mL	1.8133 mL
50 mM	-	-	-

Description

CCT137690 is a highly selective inhibitor of , and with of 15 nM, 25 nM and 19 nM. It has little effect on hERG ion-channel.

Targets

Aurora A ^[1]	Aurora C ^[1]	Aurora B ^[1]
15 nM	19 nM	25 nM

In vitro

CCT137690 displays antiproliferative activity in a range of human tumor cell lines, including SW620 colon carcinoma cell and A2780 ovarian cancer cell with GI50 of 0.3 and o.14 μM, respectively. In addition, CCT137690 also inhibit the phosphorylation of histone H3. CCT137690 inhibits the major cytochrome P450 isoforms (CYP1A2, CYP2A6, CYP2C9, CYP2C19, CYP2D6, CYP3A4) with IC50 greater than 10 μM. However, CCT137690 is a moderate inhibitor of the hERG ion-channel with IC50 of 3.0 μM. CCT137690 effectively inhibits the growth of human tumor cell lines of different origins with GI50 ranging from 0.005 to 0.47 μM. CCT137690 completely inhibits both Aurora A autophosphorylation at T288 and histone H3 phosphorylation at 0.5 μM. CCT137690 induces polyploidy, mitotic aberrations, and apoptosis in HCT116 cells. CCT137690 reduces MYCN levels and GSK3β phosphorylation in the KELLY neuroblastoma cell line. CCT137690 inhibits autophosphorylation of FLT3 and phosphorylation of its downstream targets STAT5 and p44/42 MAPK (Erk1/2).

In vivo

CCT137690 is highly orally bioavailable and inhibits the growth of SW620 colon carcinoma xenografts with no observed toxicities as defined by body weight loss. CCT137690 inhibits growth of MYCN-induced neuroblastoma at a dose of 100 mg/kg. Additionally, CCT137690 achieves target modulation and potently inhibits the growth of subcutaneous MOLM-13 xenografts, with no obvious toxicity or loss of body weight.

References

[1] Bavetsias V, et al. J Med Chem, 2010, 53(14), 5213-5228.
[2] Faisal A, et al. Mol Cancer Ther, 2011, 10(11), 2115-2123.
[3] Moore AS, et al. ASH Annu Meeting Abstr, 2010, 116, Abstr 3289.