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CCT251236

Cat. No. M13679
CCT251236 Structure
Size Price Availability Quantity
1mg USD 130  USD130 In stock
5mg USD 395  USD395 In stock
10mg USD 600  USD600 In stock
50mg USD 1750  USD1750 In stock
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Quality Control & Documentation
Biological Activity

CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an IC50 of 19 nM for inhibition of HSF1-mediated HSP72 induction.

Chemical Information
Molecular Weight 552.62
CAS Number 1693731-40-6
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Hsiao-Hui Kuo, et al. Cell Div. Heat shock factor 1 suppression induces spindle abnormalities and sensitizes cells to antimitotic drugs

[2] Samir Parekh. Clin Cancer Res. Targeting HSF1: A Prime Integrator of Proteotoxic Stress Response in Myeloma

[3] Jacqueline H L Fok, et al. Clin Cancer Res. HSF1 Is Essential for Myeloma Cell Survival and A Promising Therapeutic Target

[4] Nicola E A Chessum, et al. J Med Chem. Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766)

[5] Matthew D Cheeseman, et al. J Med Chem. Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen

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  Catalog
Abmole Inhibitor Catalog




Keywords: CCT251236 supplier, HSP, inhibitors, activators

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