Apitolisib (GDC-0980, RG-7422, GNE-390)
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 | $670 | Check With Us |
| 500mg | $999 | Check With Us |
| 1g | $1500 | Check With Us |
: Cat #: V0125 CAS #: 1032754-93-0 Purity ≥ 98%
Description: Apitolisib (formerly also known as GDC0980, RG7422, GNE390) is a novel, potent, selective and orally bioavailable class I PI3K inhibitor with potential anticancer activity.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 498.60 |
|---|---|
| Molecular Formula | C23H30N8O3S |
| CAS No. | 1032754-93-0 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 20 mg/mL (40.11 mM)r |
| Water:<1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| Solubility In Vivo | 0.5% methylcellulose+0.2% Tween 80: 30 mg/mL |
| SMILES Code | C[C@H](O)C(N1CCN(CC2=C(C)C3=NC(C4=CN=C(N)N=C4)=NC(N5CCOCC5)=C3S2)CC1)=O |
| Synonyms | Apitolisib; GDC 0980; GDC-0980; GDC0980; RG7422; RG-7422; RG 7422; GNE 390; GNE-390; GNE390 |
| Protocol | In Vitro | Apitolisib (GDC-0980) is remarkably selective for several other members of the closely related PIKK family kinases: C2alpha IC50=1300 nM; C2beta IC50=7 94 nM; VPS34 IC50=2000 nM; PI4Kalpha >10 μM; PI4Kbeta >10 μM; DNA-PK Kiapp=623 nM, respectively. |
|---|---|---|
| In Vivo | Apitolisib (GDC-0980) (1 mg/kg, p.o.) demonstrats significant efficacy in mouse xenografts and is currently in phase I clinical trials for cancer. Clearance and PPB are low, and Apitolisib (GDC-0980) shows dose-proportional exposure from 5 mg/kg dosed in PEG to 50 mg/kg dosed in suspension in MCT, a finding attributed partially to the compound’s good solubility. |
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 | 2.0056 mL | 10.0281 mL | 20.0562 mL | 40.1123 mL |
| 5mM | 0.4011 mL | 2.0056 mL | 4.0112 mL | 8.0225 mL |
| 10mM | 0.2006 mL | 1.0028 mL | 2.0056 mL | 4.0112 mL |
| 20mM | 0.1003 mL | 0.5014 mL | 1.0028 mL | 2.0056 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
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.