I-BET151 (GSK1210151A)
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 |
|---|---|---|
| 250mg | $1020 | Check With Us |
| 500mg | $1580 | Check With Us |
| 1g | $2370 | Check With Us |
: Cat #: V0412 CAS #: 1300031-49-5 Purity ≥ 98%
Description: I-BET151 (also known as GSK-1210151A) is a novel, potent and selective BET (Bromodomain and extra terminal domain) inhibitor with anticancer activity.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 415.44 |
|---|---|
| Molecular Formula | C23H21N5O3 |
| CAS No. | 1300031-49-5 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 27 mg/mL (65.0 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| SMILES Code | O=C(N1[C@@H](C2=NC=CC=C2)C)NC3=C1C4=CC(OC)=C(C5=C(C)ON=C5C)C=C4N=C3 |
| Synonyms | GSK-1210151A; GSK 1210151A; GSK1210151A; IBET-151; IBET 151; IBET151; |
| Protocol | In Vitro | I-BET151 (1 μM; 72 hours) treatment displays the majority of live cells resided in the G0 phase and commensurate with a dose- and time-dependent decrease in cell proliferation and abrogation of bromodeoxyuridine incorporation. |
|---|---|---|
| In Vivo | I-BET151 demonstrates low blood clearance in the rat (~20% liver blood flow) and good oral systemic exposure which resulted in good oral bioavailability. High clearance is observed in the dog (~95% liver blood flow). The systemic exposure in the dog is low, resulting in a poor oral bioavailability of 16%. The high blood clearance in dog correlates well with the high intrinsic clearance observed in dog microsomes and hepatocytes, whereas the low intrinsic clearances seen in rat and mouse (mouse IVC 1.6 mL/min/g; CLb 8 mL/min/kg) correlate with lower in vivo blood clearances in these species. Due to the low systemic exposure observed in the dog, I-BET151 is investigated in the mini-pig as a potential second species for toxicological evaluation where it showed low clearance (~32% liver blood flow) and good bioavailability (65%). |
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 | 2.4071 mL | 12.0354 mL | 24.0709 mL | 48.1417 mL |
| 5mM | 0.4814 mL | 2.4071 mL | 4.8142 mL | 9.6283 mL |
| 10mM | 0.2407 mL | 1.2035 mL | 2.4071 mL | 4.8142 mL |
| 20mM | 0.1204 mL | 0.6018 mL | 1.2035 mL | 2.4071 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
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Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start)
×
Volume(start)
=
Concentration(final)
×
Volume(final)
This equation is commonly abbreviated as: C1 V1 = C2 V2
Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
Number of animals
Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
DMSO(Master liquid concentration
mg/mL)
,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
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.
- (2) Be sure to add the solvent(s) in order.