2. PI3K/Akt/mTOR Apoptosis
  3. PI3K mTOR Apoptosis
  4. Apitolisib

Apitolisib  (Synonyms: GDC-0980; GNE 390; RG 7422)

製品番号: HY-13246 純度: 99.29%
COA 取扱説明書 Technical Support

Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a?Ki?of 17 nM for mTOR.

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Apitolisib

Apitolisib 構造式

CAS 番号 : 1032754-93-0

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 84 在庫あり
Solution
10 mM * 1 mL in DMSO USD 84 在庫あり
Solid
5 mg $77 在庫あり
10 mg $110 在庫あり
50 mg $319 在庫あり
100 mg $539 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 13 publication(s) in Google Scholar

Other Forms of Apitolisib:

Apitolisib 関連抗体

Top Publications Citing Use of Products

PI3K アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

mTOR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
mTOR mTORC1 mTORC2

  • 生物活性

  • プロトコル

  • 純度とドキュメンテーション

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製品説明

Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a?Ki?of 17 nM for mTOR.

IC50 & Target[2]

PI3Kα

5 nM (IC50)

PI3Kδ

7 nM (IC50)

PI3Kγ

14 nM (IC50)

PI3Kβ

27 nM (IC50)

mTOR

17 nM (Ki)

TORC1

 

TORC2

 

Cellular Effect
Cell Line Type Value Description References
HCC1937 IC50
3.21 μM
Compound: GDC-0980
Antiproliferative activity against human BRCA-1 deficient HCC1937 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay
Antiproliferative activity against human BRCA-1 deficient HCC1937 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay
[PMID: 33740547]
HCT-116 IC50
1.11 μM
Compound: GDC-0980
Antiproliferative activity against human BRCA-2 deficient HCT-116 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay
Antiproliferative activity against human BRCA-2 deficient HCT-116 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay
[PMID: 33740547]
MDA-MB-231 IC50
2.46 μM
Compound: GDC-0980
Antiproliferative activity against human BRCA proficient MDA-MB-231 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay
Antiproliferative activity against human BRCA proficient MDA-MB-231 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay
[PMID: 33740547]
MDA-MB-468 IC50
1.67 μM
Compound: GDC-0980
Antiproliferative activity against human BRCA proficient MDA-MB-468 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay
Antiproliferative activity against human BRCA proficient MDA-MB-468 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay
[PMID: 33740547]
PC-3 EC50
0.31 μM
Compound: 3
Antiproliferative activity against human PC3 cells after 3 days by CellTitre-Glo assay
Antiproliferative activity against human PC3 cells after 3 days by CellTitre-Glo assay
[PMID: 27096040]
PC-3 IC50
307 nM
Compound: 2, GDC-0980
Antiproliferative activity against human PC3 cells after overnight incubation by CellTiter-Glo luminescence assay
Antiproliferative activity against human PC3 cells after overnight incubation by CellTiter-Glo luminescence assay
[PMID: 21981714]
PC-3 IC50
36 nM
Compound: 2, GDC-0980
Inhibition of PIK3 gamma-mediated Akt phosphorylation at Ser473 in human PC3 cells by ELISA
Inhibition of PIK3 gamma-mediated Akt phosphorylation at Ser473 in human PC3 cells by ELISA
[PMID: 21981714]
SW-620 IC50
1.72 μM
Compound: GDC-0980
Antiproliferative activity against human BRCA-2 proficient SW-620 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay
Antiproliferative activity against human BRCA-2 proficient SW-620 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay
[PMID: 33740547]
体外実験

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[1]. A recent study shows that Apitolisib (GDC-0980) reduces cancer cell viability by inhibiting cell-cycle procession and inducing apoptosis with most potency in prostate (IC50 < 200 nM 50%), <500 nM 100%), breast (IC50 <200 nM 37%, <500 nM 78%) and NSCLC lines (IC50 <200 nM 29%, <500 nM 88%) and less potency in pancreatic (IC50 <200 nM 13%, <500 nM 67%) and melanoma cell lines (IC50 <200 nM 0%, <500 nM 33%)[2].

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

Apitolisib 関連抗体
体内実験

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[1]. Apitolisib (GDC-0980) (5 mg/kg, p.o.) results in greater than 50% TGI in 15 of the 20 xenograft models. The difference in tumor response to Apitolisib (GDC-0980) treatment correlates with the duration of knockdown of pAkt/tAkt[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

498.60

分子式

C23H30N8O3S
CAS 番号
Appearance

Solid

Color

White to yellow

SMILES

C[C@@H](C(N1CCN(CC1)CC2=C(C3=NC(C4=CN=C(N=C4)N)=NC(N5CCOCC5)=C3S2)C)=O)O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 14.29 mg/mL (28.66 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 2.0056 mL 10.0281 mL 20.0562 mL
5 mM 0.4011 mL 2.0056 mL 4.0112 mL
10 mM 0.2006 mL 1.0028 mL 2.0056 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.43 mg/mL (2.87 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.43 mg/mL (2.87 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.29%

COA (249 KB) LCMS (89 KB)

取扱説明書 (2659 KB)
参考文献
キナーゼ実験
[2]

Ten centimeter square dishes are seeded with 2 million cells in a volume of 10 mL followed by incubation at 37°C under 5% CO2 overnight (appr 16 hours). Cells are treated with the indicated concentration of GDC-0941, Apitolisib (GDC-0980), or mTOR1/2 inhibitor for the time indicated. Following treatment, cells are washed with cold PBS and lysed in 1X Cell Extraction Buffer, 1 mM PMSF, and Phosphatase Inhibitor Cocktails 1 and 2 are all needed. Protein concentration is determined using the Pierce BCA Protein Assay Kit. For immunoblots, equal protein amounts are separated by electrophoresis through NuPage Bis-Tris 10% gradient gels; proteins are transferred onto polyvinylidene difluoride membranes using the Criterion system and protocol.

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
細胞実験
[2]

Three hundred and eighty-four-well plates are seeded with 2,000 cells/well in a volume of 54 μL per well followed by incubation at 37°C under 5% CO2 overnight (appr 16 hours). Compounds are diluted in dimethyl sulfoxide to generate the desired stock concentrations then added in a volume of 6 μL per well. All treatments are tested in quadruplicate. After 4 days incubation, relative numbers of viable cells are estimated using CellTiter-Glo and total luminescence is measured on a Wallac Multilabel Reader. The concentration of drug resulting in 50% inhibition of cell viability (IC50) or 50% maximal effective concentration (EC50) is determined using Prism software. For cell lines that failed to achieve an IC50 the highest concentration tested (20 μM) is listed.

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
動物実験
[1]

Human prostate cancer PC3 cells are resuspended in Hank’s Balanced Salt Solution and 3×106 cells implanted subcutaneously into the right hind flank of athymic nu/nu (nude) mice. Tumors are monitored until they reach a mean tumor volume of 150-200 mm3 prior to the initiation of dosing. MCF7.1 cells resuspended in a 1:1 mixture of Hank’s Buffered Salt Solution and Matrigel Basement Membrane Matrix are 5×106 subcutaneously implanted into the right hind flank of athymic nu/nu (nude) mice. Prior to cell inoculation, 17β-estradiol (0.36 mg/pellet, 60-day release, no. SE-121) are implanted into the dorsal shoulder blade area of each nude mouse. After implantation of cells, tumors are monitored until they reach a mean tumor volume of 250-350 mm3 prior to initiating dosing. Compound 2 is dissolved in 0.5% methylcellulose with 0.2% Tween-80 (MCT). Female nude (nu/nu) mice that are 6-8 weeks old and weighed 20-30 g are obtained from Charles River Laboratories. Tumor bearing mice are dosed daily for 14-21 days depending on the xenograft model with 100 μL of vehicle (MCT) or test agent orally.

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0056 mL 10.0281 mL 20.0562 mL 50.1404 mL
5 mM 0.4011 mL 2.0056 mL 4.0112 mL 10.0281 mL
10 mM 0.2006 mL 1.0028 mL 2.0056 mL 5.0140 mL
15 mM 0.1337 mL 0.6685 mL 1.3371 mL 3.3427 mL
20 mM 0.1003 mL 0.5014 mL 1.0028 mL 2.5070 mL
25 mM 0.0802 mL 0.4011 mL 0.8022 mL 2.0056 mL
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Apitolisib Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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.

Keywords:

Apitolisib1032754-93-0GDC-0980 GNE 390 RG 7422GDC0980GDC 0980GNE390GNE 390GNE-390RG7422RG 7422RG-7422PI3KmTORApoptosisPhosphoinositide 3-kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

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製品番号:
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