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

Risovalisib (CYH33) is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. Risovalisib inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. Risovalisib has potent activity against solid tumors.

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Risovalisib Chemical Structure

Risovalisib Chemical Structure

CAS No. : 1494684-28-4

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Based on 1 publication(s) in Google Scholar

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Description

Risovalisib (CYH33) is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. Risovalisib inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. Risovalisib has potent activity against solid tumors[1][2][3].

IC50 & Target[1]

PI3Kα

5.9 nM (IC50)

PI3Kβ

598 nM (IC50)

PI3Kδ

78.7 nM (IC50)

PI3Kγ

225 nM (IC50)

In Vitro

Risovalisib (CYH33) inhibits cell proliferation with IC50s below 1 μM in 56% (18/32) of the breast cancer cell lines[2].
CYH33 (0.012-1 μM; for 24 hours) significantly arrests T47D and MCF7 cells in G1 phase in a concentration-dependent manner[2].
CYH33 (4-1000 nM; 1 hour) concurrently inhibits phosphorylation of ERK and Akt in both T47D and MCF7 cells[2].
CYH33 (0.11-1 μM; 24 hours) fails to induce apoptosis in MCF7 and MDA-MB-231 cells[2].

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

Cell Cycle Analysis[2]

Cell Line: Sensitive T47D, MCF7 and resistant MDA-MB-231 cells
Concentration: 0.012, 0.037, 0.11, 0.33, 1 μM
Incubation Time: For 24 hours
Result: Arrested T47D and MCF7 cells in G1 phase in a concentration-dependent manner, accompanied with concomitant reduced cell population in S phase.
Had little effect on cell cycle distribution in resistant MDA-MB-231 cells.

Western Blot Analysis[2]

Cell Line: Sensitive T47D, MCF7 and resistant MDA-MB-231 cells
Concentration: 4, 12, 37, 111, 333, 1000 nM
Incubation Time: 1 hour
Result: Concurrently inhibited phosphorylation of ERK and Akt in both T47D and MCF7 cells, whereas it had little effect on phosphorylated ERK (pERK) in MDA-MB-231 cells up to 1 μM.
In Vivo

Risovalisib (CYH33) (2-20 mg/kg; oral; once a day for 21 days) potently restrains tumor growth in mice bearing human breast cancer cell xenografts[2].
Single administration of CYH33 (20 mg/kg; oral) significantly down-regulates the level of phosphorylated Akt in tumor tissues, demonstrating the suppression of PI3K signaling in nude mice[2].
CYH33 (10 mg/kg; oral; once a day for 18-d or 20-d respectively) delays the restoration of blood glucose and area under the curve (AUC) of blood glucose increased upon CYH33 treatment in T47D xenografts and R26-Pik3caH1047R;MMTV-Cre mice[2].

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

Animal Model: SCID mice aged 4-6 weeks bearing human breast cancer T47D xenografts[2]
Dosage: 2, 5, 10, 20 mg/kg
Administration: Oral; once a day for 21 days
Result: Displayed marginal inhibitory effect on the tumor growth at lower doses (2 and 5 mg/kg) and significantly attenuated tumor growth at the dose of 10 or 20 mg/kg, yielding T/C values of 58.36% and 49.42% respectively.
Clinical Trial
Molecular Weight

598.60

Formula

C24H29F3N8O5S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(OC)NC1=NC=C(C(N=C2N3CCOCC3)=NN4C2=CC(CN5CCN(S(=O)(C)=O)CC5)=C4)C(C(F)(F)F)=C1

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 : 50 mg/mL (83.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6706 mL 8.3528 mL 16.7056 mL
5 mM 0.3341 mL 1.6706 mL 3.3411 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6706 mL 8.3528 mL 16.7056 mL 41.7641 mL
5 mM 0.3341 mL 1.6706 mL 3.3411 mL 8.3528 mL
10 mM 0.1671 mL 0.8353 mL 1.6706 mL 4.1764 mL
15 mM 0.1114 mL 0.5569 mL 1.1137 mL 2.7843 mL
20 mM 0.0835 mL 0.4176 mL 0.8353 mL 2.0882 mL
25 mM 0.0668 mL 0.3341 mL 0.6682 mL 1.6706 mL
30 mM 0.0557 mL 0.2784 mL 0.5569 mL 1.3921 mL
40 mM 0.0418 mL 0.2088 mL 0.4176 mL 1.0441 mL
50 mM 0.0334 mL 0.1671 mL 0.3341 mL 0.8353 mL
60 mM 0.0278 mL 0.1392 mL 0.2784 mL 0.6961 mL
80 mM 0.0209 mL 0.1044 mL 0.2088 mL 0.5221 mL
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Risovalisib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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