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GDC-0980 (RG7422)

Class I PI3K inhibitor for PI3Kα/β/δ/γ CAS# 1032754-93-0

GDC-0980 (RG7422)

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GDC-0980 (RG7422): 5mg $69 In Stock
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Chemical structure

GDC-0980 (RG7422)

3D structure

Chemical Properties of GDC-0980 (RG7422)

Cas No. 1032754-93-0 SDF Download SDF
PubChem ID 25254071 Appearance Powder
Formula C23H30N8O3S M.Wt 498.61
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Apitolisib; GNE 390; RG 7422
Solubility DMSO : 14.29 mg/mL (28.66 mM; Need ultrasonic)
Chemical Name (2S)-1-[4-[[2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2-hydroxypropan-1-one
SMILES CC1=C(SC2=C1N=C(N=C2N3CCOCC3)C4=CN=C(N=C4)N)CN5CCN(CC5)C(=O)C(C)O
Standard InChIKey YOVVNQKCSKSHKT-HNNXBMFYSA-N
Standard InChI InChI=1S/C23H30N8O3S/c1-14-17(13-29-3-5-31(6-4-29)22(33)15(2)32)35-19-18(14)27-20(16-11-25-23(24)26-12-16)28-21(19)30-7-9-34-10-8-30/h11-12,15,32H,3-10,13H2,1-2H3,(H2,24,25,26)/t15-/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of GDC-0980 (RG7422)

DescriptionApitolisib (GDC-0980, RG7422) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 values of 5 nM/27 nM/7 nM/14 nM, respectively.
Targetsp110αp110δp110γmTORp110β  
IC505 nM7 nM14 nM17 nM(Ki app)27 nM  

Protocol

Kinase Assay [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, 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.

Cell Assay [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.

Animal Administration [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.

References:
[1]. Sutherlin DP, et al. Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer. J Med Chem, 2011, 54(21), 7579-7587. [2]. Wallin JJ, et al. GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway. Mol Cancer Ther, 2011, 10(12), 2426-2436.

GDC-0980 (RG7422) Dilution Calculator

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Preparing Stock Solutions of GDC-0980 (RG7422)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.0056 mL 10.0279 mL 20.0558 mL 40.1115 mL 50.1394 mL
5 mM 0.4011 mL 2.0056 mL 4.0112 mL 8.0223 mL 10.0279 mL
10 mM 0.2006 mL 1.0028 mL 2.0056 mL 4.0112 mL 5.0139 mL
50 mM 0.0401 mL 0.2006 mL 0.4011 mL 0.8022 mL 1.0028 mL
100 mM 0.0201 mL 0.1003 mL 0.2006 mL 0.4011 mL 0.5014 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on GDC-0980 (RG7422)

GDC-0980 (RG7422) is a selective, novel, potent and orally bioavailable inhibitor of class 1 PI3K/mTOR kinase with the Ki value of 17nmol/L for mTOR kinase [1].

GDC-0980 (RG7422) has shown the effective inhibition with the IC50 values of <200nmol/L in prostate, breast and NSCLC lines, respectinely. In addition, GDC-0980 (RG7422) has been reported to reduce cell viability in KPL4 cells by cell-cycle inhibition and induction of apoptosis with the IC50 value of 109nM and the EC50 value of 78nM. Furthermore, GDC-0980 (RG7422) has been revealed to significantly inhibit tumor responses in xenograft models in oral dose of the compound. Besides, GDC-0980 (RG7422) has been noted to enhance the antitumor activity in combination with antitumor agents ( docetaxel) in vivo [1].

References:
[1] Wallin JJ1, Edgar KA, Guan J, Berry M, Prior WW, Lee L, Lesnick JD, Lewis C, Nonomiya J, Pang J, Salphati L, Olivero AG, Sutherlin DP, O'Brien C, Spoerke JM, Patel S, Lensun L, Kassees R, Ross L, Lackner MR, Sampath D, Belvin M, Friedman LS. GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway. Mol Cancer Ther. 2011 Dec;10(12):2426-36. doi: 10.1158/1535-7163.MCT-11-0446. Epub 2011 Oct 13.

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Description

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.

Keywords:

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