1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
  2. HSP
  3. CCT251236

CCT251236 

Cat. No.: HY-101026 Purity: 99.03%
Handling Instructions

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.

For research use only. We do not sell to patients.

CCT251236 Chemical Structure

CCT251236 Chemical Structure

CAS No. : 1693731-40-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 481 In-stock
Estimated Time of Arrival: December 31
1 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 396 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

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.

IC50 & Target[1]

HSP72

19 nM (IC50, SK-OV-3 cells)

In Vitro

CCT251236 displays the desired balance of in vitro properties, while maintaining excellent cellular activity with an IC50 of 19 nM. The free GI50 in SK-OV-3 cells is 1.1 nM. Western blotting confirms that CCT251236 blocks the HSF1-mediated induction of both HSP72 and HSP27 as representative heat shock proteins, following treatment with the HSP90 inhibitor 17AAG. Also, qPCR analysis demonstrates that CCT251236 inhibits the induction of HSP72 at the mRNA level, clearly blocking the induction of HSPA1A gene expression with an IC50 of 40 nM[1].

In Vivo

CCT251236 possesses low total blood clearance (10% hepatic blood flow) and moderate oral bioavailability, with a half-life sufficient to allow once-a-day dosing. Clear therapeutic efficacy is observed with CCT251236, with a tumor growth inhibition of 70% based on final tumor volumes[1].

Molecular Weight

552.62

Formula

C₃₂H₃₂N₄O₅

CAS No.

1693731-40-6

SMILES

CC1=CC=C(NC(C2=CC(OCCO3)=C3C=C2)=O)C=C1NC(C4=CC(C=CC(OCCN5CCCC5)=N6)=C6C=C4)=O

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 150 mg/mL (271.43 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8096 mL 9.0478 mL 18.0956 mL
5 mM 0.3619 mL 1.8096 mL 3.6191 mL
10 mM 0.1810 mL 0.9048 mL 1.8096 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Mice: SK-OV-3 cells are injected subcutaneously into athymic mice for tumor formation. Once tumors are established, the mice are randomized into treatment and control groups and are dosed orally once-a-day with either vehicle or 20 mg/kg of CCT251236. Tumor volumes and mouse body weights are measured throughout and tumor weights are measured at the end of the study, while total tumor concentrations are measured 2 and 6 hours post final dose[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Product Name:
CCT251236
Cat. No.:
HY-101026
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