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CCT137690

Cat. No. M2103
CCT137690 Structure
Size Price Availability Quantity
10mg USD 120  USD120 In stock
50mg USD 420  USD420 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

CCT137690 is a highly selective, orally bioavailable Aurora kinase inhibitor that inhibits Aurora A and B kinases with low nanomolar IC50 values in both biochemical and cellular assays. CCT137690 inhibits histone H3 and transforming acidic coiled-coil 3 phosphorylation (Aurora B and Aurora A substrates, respectively) in HCT116 and HeLa cells efficiently. CCT137690 displays antiproliferative activity in a range of human tumor cell lines. CCT137690 treatment of MYCN-amplified neuroblastoma cell lines inhibits cell proliferation and decreases MYCN protein expression.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 551.48
Formula C26H31BrN8O
CAS Number 1095382-05-0
Purity >98%
Solubility DMSO
Storage at -20°C
References

[1] Moore AS, et al. Leukemia. Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns.

[2] Faisal A, et al. Mol Cancer Ther. The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo.

[3] Bavetsias V, et al. J Med Chem. Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate.

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Keywords: CCT137690 supplier, Aurora Kinase, inhibitors
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