CH5132799
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 | $1340 | Check With Us |
| 500mg | $1950 | Check With Us |
| 1g | $2925 | Check With Us |
: Cat #: V0138 CAS #: 1007207-67-1 Purity ≥ 98%
Description: CH5132799 is a novel and potent class I PI3K (phosphoinositide 3-kinase) inhibitor with potential anticancer activity.
Top Publications Citing Invivochem Products
Publications Citing InvivoChem Products
Product Promise
- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 377.42 |
|---|---|
| Molecular Formula | C15H19N7O3S |
| CAS No. | 1007207-67-1 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 12 mg/mL (31.79 mM)r |
| Water:<1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| Solubility In Vivo | 1% DMSO+30% polyethylene glycol+1% Tween 80: 30mg/mL |
| SMILES Code | NC1=NC=C(C2=C3C(N(S(=O)(C)=O)CC3)=NC(N4CCOCC4)=N2)C=N1 |
| Synonyms | CH5132799; CH-5132799; CH 5132799; PA-799; PA799; PA-799; Izorlisib |
| Protocol | In Vitro | Izorlisib (CH5132799) is a selective class I PI3K inhibitor with potent antitumor activity against tumors harboring the PIK3CA mutations. Izorlisib selectively inhibits class I PI3Ks and PI3Kα mutants in in vitro kinase assays. Izorlisib inhibits class I PI3Ks, particularly PI3Kα, with an IC50 of 14 nM. IC50 values against class II PI3Ks (C2α and C2β), a class III PI3K (Vps34), and a class IV PI3K (mTOR) are more than 100-fold higher than that against PI3Kα. Interestingly, slightly lower IC50 values are observed against PI3Kα with oncogenic mutations E542K, E545K, and H1047R than against wild-type (WT) PI3Kα. In an analysis of cocrystal structure with PI3Kγ (PBD ID: 3APC), Izorlisib is shown to interact with ATP-binding sites of the enzyme, suggesting an ATP competitive mode of inhibition. No significant inhibitory activities of Izorlisib are observed against a representative panel of 26 protein kinases, including RTKs, nonreceptor tyrosine kinases, and serine/threonine kinases. These data indicate that Izorlisib is a selective class I PI3K inhibitor, especially against PI3Kα and its mutants. Izorlisib shows superior antiproliferative activity across the 4 tumor types, with 75% (45/60) of lines having an IC50 below 1 μM and 38% (23/60) of lines having an IC50 below 0.3 μM. |
|---|---|---|
| In Vivo | Mice bearing BT-474 tumors (n=14) are orally administered 50 mg/kg of Everolimus on a daily basis for 31 days and then randomized. After randomization, the mice are orally administered 50 mg/kg of Everolimus (n=4) and 12.5 mg/kg (n=5), and 25 mg/kg (n=5) of Izorlisib on a daily basis for 7 days. C, the vehicle-, Everolimus, and CH5132799-treated (25 mg/kg) tumors are resected at 4 hours after terminal administration in B, lysed, and analyzed by Western blotting. Izorlisib administration leads to a remarkable regression in a dose-dependent manner of the tumors regrown after the long-term Everolimus treatment. The tumors are resected at the end of treatment and analyzed by Western blotting with respect to PI3K pathway inhibition. Izorlisib suppresses various effectors in the PI3K pathway, including Akt, FoxO1, S6K, S6, and 4E-BP1, whereas Everolimus inhibits only phosphorylation of S6K and S6, both downstream effectors of mTORC1. |
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 | 2.6496 mL | 13.2478 mL | 26.4957 mL | 52.9914 mL |
| 5mM | 0.5299 mL | 2.6496 mL | 5.2991 mL | 10.5983 mL |
| 10mM | 0.2650 mL | 1.3248 mL | 2.6496 mL | 5.2991 mL |
| 20mM | 0.1325 mL | 0.6624 mL | 1.3248 mL | 2.6496 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.