(+)-JQ1
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 500mg | $400 | In Stock |
| 1g | $600 | In Stock |
| 5g | $900 | In Stock |
: Cat #: V0411 CAS #: 1268524-70-4 Purity ≥ 98%
Description: (+)-JQ1 is a novel, potent and highly specific BET (Bromodomain and extra terminal domain) bromodomain inhibitor with antineoplastic activity.
References: Filippakopoulos P, et al. Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73.
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| Molecular Weight (MW) | 456.99 |
|---|---|
| Molecular Formula | C23H25ClN4O2S |
| CAS No. | 1268524-70-4 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 91 mg/mL (199.1 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 91 mg/mL (199.1 mM) | |
| Solubility In Vivo | 2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5 mg/mL |
| SMILES Code | O=C(OC(C)(C)C)C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N1 |
| Synonyms | Bromodomain Inhibitor; (+)-JQ 1; (+)-JQ-1; (+)-JQ1; |
| Protocol | In Vitro | (+)-JQ-1 represents a potent, highly specific and Kac competitive inhibitor for the BET family of bromodomains. (+)-JQ-1 (100 nM, 48 h) prompts squamous differentiation exhibited by cell spindling, flattening and increased expression of keratin. (+)-JQ-1 (250 nM) induces rapid expression of keratin in treated NMC 797 cells compared to (-)-JQ1 (250 nM) and vehicle controls, as determined by quantitative immunohistochemistry.(+)-JQ-1 (250 nM) elicits a time-dependent induction of strong (3+) keratin staining of treated NMC 797 cells, compared to (-)-JQ1 (250 nM). |
|---|---|---|
| In Vivo | Matched cohorts of mice with established tumors are randomized to treatment with (+)-JQ1 (50 mg/kg) or vehicle, administered by daily intraperitoneal injection. Prior to randomization, and after four days of therapy, mice are evaluated by FDG-PET imaging. A marked reduction in FDG uptake is observed with (+)-JQ1 treatment. Tumor-volume measurements confirm a reduction in tumor growth with JQ1 treatment. Pharmacokinetic studies of (+)-JQ1 are performed in CD1 mice following intravenous and oral administration. Mean plasma concentration-time profiles of (+)-JQ1 after intravenous dosing (5 mg/kg). The pharmacokinetic parameters for intravenous (+)-JQ1 demonstrate excellent drug exposure (AUC=2090 hr*ng/mL) and an approximately one hour half-life (T1/2). Mean plasma concentration-time profiles of (+)-JQ1 after oral dosing (10 mg/kg). The pharmacokinetic parameters for oral (+)-JQ1 demonstrate excellent oral bioavailability (F=49%), peak plasma concentration (Cmax=1180 ng/mL) and drug exposure (AUC=2090 hr*ng/mL). |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.1882 mL | 10.9412 mL | 21.8823 mL | 43.7646 mL |
| 5mM | 0.4376 mL | 2.1882 mL | 4.3765 mL | 8.7529 mL |
| 10mM | 0.2188 mL | 1.0941 mL | 2.1882 mL | 4.3765 mL |
| 20mM | 0.1094 mL | 0.5471 mL | 1.0941 mL | 2.1882 mL |
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Step Two: Enter the in vivo formulation
%DMSO
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%ddH2O
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Method for preparing DMSO master liquid:
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,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
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DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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