1. PI3K/Akt/mTOR
  2. PI3K
  3. CH5132799

CH5132799 

Cat. No.: HY-15466 Purity: >98.0%
Handling Instructions

CH5132799 is a selective class I PI3K inhibitor. CH5132799 inhibits class I PI3Ks, particularly PI3Kα, with an IC50 of 14 nM.

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

CH5132799 Chemical Structure

CH5132799 Chemical Structure

CAS No. : 1007207-67-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 238 In-stock
Estimated Time of Arrival: December 31
5 mg USD 216 In-stock
Estimated Time of Arrival: December 31
10 mg USD 336 In-stock
Estimated Time of Arrival: December 31
50 mg USD 936 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1320 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE CH5132799

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

CH5132799 is a selective class I PI3K inhibitor. CH5132799 inhibits class I PI3Ks, particularly PI3Kα, with an IC50 of 14 nM.

IC50 & Target[1]

PI3Kα

14 nM (IC50)

PI3Kα-H1047R

5.6 nM (IC50)

PI3Kα-E545K

6.7 nM (IC50)

PI3Kα-E542K

6.7 nM (IC50)

PI3Kγ

36 nM (IC50)

PI3Kβ

120 nM (IC50)

PI3Kδ

500 nM (IC50)

PI3KC2β

5.3 μM (IC50)

mTOR

1.6 μM (IC50)

In Vitro

CH5132799 is a selective class I PI3K inhibitor with potent antitumor activity against tumors harboring the PIK3CA mutations. CH5132799 selectively inhibits class I PI3Ks and PI3Kα mutants in in vitro kinase assays. CH5132799 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), CH5132799 is shown to interact with ATP-binding sites of the enzyme, suggesting an ATP competitive mode of inhibition. No significant inhibitory activities of CH5132799 are observed against a representative panel of 26 protein kinases, including RTKs, nonreceptor tyrosine kinases, and serine/threonine kinases. These data indicate that CH5132799 is a selective class I PI3K inhibitor, especially against PI3Kα and its mutants. CH5132799 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[1].

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 CH5132799 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. CH5132799 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. CH5132799 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[1].

Clinical Trial
Molecular Weight

377.42

Formula

C₁₅H₁₉N₇O₃S

CAS No.

1007207-67-1

SMILES

NC1=NC=C(C2=C3C(N(S(=O)(C)=O)CC3)=NC(N4CCOCC4)=N2)C=N1

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 : 4.55 mg/mL (12.06 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6496 mL 13.2478 mL 26.4957 mL
5 mM 0.5299 mL 2.6496 mL 5.2991 mL
10 mM 0.2650 mL 1.3248 mL 2.6496 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 0.46 mg/mL (1.22 mM); Clear solution

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

The cell lines are added to the wells of 96-well plates containing 0.076 to 10,000 nM CH5132799 and incubated at 37°C. After 4 days of incubation, Cell Counting Kit-8 solution is added and, after incubation for several more hours, absorbance at 450 nm is measured with Microplate-Reader iMark. The antiproliferative activity is calculated. The IC50 values are calculated[1].

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

Animal Administration
[1]

Mice[1]
Female BALB-nu/nu mice (CAnN.Cg-Foxn1/CrlCrlj nu/nu) are used. A total of 4×106 to 1.2×107 cells are suspended in 100 to 200 μL serum-free culture medium and injected subcutaneously into the right flank of the mice. Tumor size is measured by using a gauge twice per week, and tumor volume (TV) is calculated. Once the tumors reach a volume of approximately 200 to 300 mm3, animals are randomized into groups (n=4 or 5 in each group) and treatment is initiated. CH5132799 and Everolimus are orally administered once a day and Trastuzumab is intravenously injected once a week.

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

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

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: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CH5132799
Cat. No.:
HY-15466
Quantity: