Afuresertib (GSK2110183)

Name: Afuresertib (GSK2110183)
Brand: Selleck Chemicals
SKU: S7521
Rating: 5 (14 reviews)

For research use only.

Catalog No.S7521

14 publications

Afuresertib (GSK2110183) Chemical Structure

CAS No. 1047644-62-1

Afuresertib (GSK2110183) is a potent, orally bioavailable Akt inhibitor with K_i of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.

Selleck's Afuresertib (GSK2110183) has been cited by 14 publications

Nat Chem Biol, 2017, 13(3):333-338

PubMed: 28114274 ( click the link to review the publication )

Nat Commun, 2020, 11(1):4629

PubMed: 32934208 ( click the link to review the publication )

Cell Oncol (Dordr), 2020, 8

PubMed: 32382996 ( click the link to review the publication )

Cancer Sci, 2020, 111(5):1663-1675

PubMed: 32176823 ( click the link to review the publication )

Hum Cell, 2020, 33(4):1197-1203

PubMed: 32851605 ( click the link to review the publication )

Blood Adv, 2020,

PubMed: 32898245 ( click the link to review the publication )

Nat Commun, 2019, 10(1):95

PubMed: 30626865 ( click the link to review the publication )

Cancers (Basel), 2019, 22;11(7):1029

PubMed: 31336622 ( click the link to review the publication )

Toxicol Appl Pharmacol, 2019, 381:114729

PubMed: 31445927 ( click the link to review the publication )

J Clin Invest, 2018, 128(10):4604-4621

PubMed: 30106752 ( click the link to review the publication )

Clin Cancer Res, 2018, 24(24):6408-6420

PubMed: 30126942 ( click the link to review the publication )

Cell Death Dis, 2018, 9(9):911

PubMed: 30185800 ( click the link to review the publication )

Oncol Lett, 2018, 15(6):9450-9456

PubMed: 29928335 ( click the link to review the publication )

Nucleic Acids Res, 2017, 45(16):9654-9678

PubMed: 28934469 ( click the link to review the publication )

1 Customer Review

Analysis of the mechanism of action of the enhanced anti‑tumor effect of the combination therapy of suboptimal doses of pomalidomide plus dexamethasone and afuresertib in MM cells. (A‑C) The altered expression of protein substrates was analyzed in two MM cell lines that were treated with suboptimal doses of PD, or AFU, or the PD and AFU combination. The XG‑7 and U266 cell lines were subjected to the indicated treatments for 48 and 72 h, respectively. (A) Caspases, (B) substrates related mainly to the working mechanism of IMiDs, (C) substrates mainly related to the working mechanism of afuresertib, and (D) two primary MM cell cultures, were subjected to the analysis in the same manner as the two MM cell lines. In the expression panel of p‑FoxO3a/FoxO1, the upper band represents p‑FoxO3a and the lower band represents p‑FOXO1. PD, pomalidomide plus dexamethasone; AFU, Afuresertib; MM, multiple myeloma; IMiDs, immunomodulatory drugs.

ONCOLOGY LETTERS, 2018, https://doi.org/10.3892/ol.2018.8501. Afuresertib (GSK2110183) purchased from Selleck.

Purity & Quality Control

Choose Selective Akt Inhibitors

Biological Activity

Description

Afuresertib (GSK2110183) is a potent, orally bioavailable Akt inhibitor with K_i of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.

Targets

Akt1 ^[1] (Cell-free assay)	Akt2 ^[1] (Cell-free assay)	Akt3 ^[1] (Cell-free assay)
0.08 nM(Ki)	2 nM(Ki)	2.6 nM(Ki)

In vitro

Afuresertib inhibits the kinase activity of the E17K AKT1 mutant protein with EC50 of 0.2 nM. Afuresertib shows a concentration-dependent effect on multiple AKT substrate phosphorylation levels, including GSK3b, PRAS40, FOXO and Caspase 9. Overall 65% of the hematological cell lines are sensitive to afuresertib (EC50 < 1 μM). Among tested solid tumor cell lines, 21% have EC50 < 1 μM in response to afuresertib.^[1]

Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
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Sf9	MmLjSpVv[3Srb36gZZN{[Xl?	NHrGZYo1OCCvaX7z	NF;n[ppKdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJIh2dWGwIFHLWFMh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5ic4Xid5Rz[XSnIIDoc5NxcG:{eXzheIlwdiC3c3nu[{BjcW:2aX6tZYh5NUGUS2LFVmF[W0[JSFjBMYFucWSnIIP1ZpN1emG2ZTDhcoQhY2ejbX3hMVM{WF2DVGCgbY5kfWKjdHXkJIZweiB2MDDtbY5{KGK7IITvdEBkd3WwdDDtbYNzd3CuYYTlJJNkcW62aXzsZZRqd25iY3;1cpRqdmdibXX0bI9lNCCLQ{WwJF0hOC5yMEG1PFUh\|ryPLh?=	NIrneWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOjF7NEKyM{c,S2iHTVLMQE9iRg>?
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Sf9	MlzlSpVv[3Srb36gZZN{[Xl?	M{nBfVQxKG2rboO=	MX3Jcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIHj1cYFvKEGNVEKg[ZhxemW\|c3XkJIlvKFOoOTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4he3Wkc4TyZZRmKHCqb4PwbI9zgWyjdHnvckB2e2mwZzDibY91cW5vYXj4MWFTU1KHUlHZV2ZIUEiDLXHtbYRmKHO3YoP0doF1\SCjbnSgX4didW2jLUOzVH1CXFBiaX7jeYJifGWmIH\vdkA1OCCvaX7zJIJ6KHSxcDDjc5VvfCCvaXPyc5Bt[XSnIIPjbY51cWyuYYTpc44h[2:3boTpcochdWW2aH;kMEBKSzVyIE2gNE4xOSEQvF2u	M{j5bFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIzOTl2MkKvK\|5EcEWPQly8M4E,
MV522	MoTBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NHnBTHA4OiCqcoO=	NWHkWHE{T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVVZ3MkKgZ4VtdHNiYYSgNVoyOCCvb3zhdkBz[XSrbzDv[kBkd22yb4Xu[EBqdiCycnXz[Y5k\SCxZjDOMZs{NVt\|LXP5Z4xweHKxcInsMVUuMDJvZnz1c5JwNTRvaX;kc{1xcGWweXzhcYlvdylvNjy4MYRqdWW2aInsMUAzNDRuNz30dolwgG9vMzy0MFYtPy22ZYTyZYh6\HKxLULIMZB6emmmb2u0MFMu\F2yeYLpcYllcW5vMT35cH1xcGWweXz9ZYNmfGGvaXTlJIlv[3WkYYTl[EBnd3JiN{KgbJJ{NCCLQ{WwJF0hOC5yMUKg{txONg>?	MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNlE6PDJ{Lze+R4hGVUKOPD;hQi=>
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NCI-H727	NWe0dFhKT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MX[3NkBpenN?	MmXSS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUmNKNUh5MkegZ4VtdHNiYYSgNVoyOCCvb3zhdkBz[XSrbzDv[kBkd22yb4Xu[EBqdiCycnXz[Y5k\SCxZjDOMZs{NVt\|LXP5Z4xweHKxcInsMVUuMDJvZnz1c5JwNTRvaX;kc{1xcGWweXzhcYlvdylvNjy4MYRqdWW2aInsMUAzNDRuNz30dolwgG9vMzy0MFYtPy22ZYTyZYh6\HKxLULIMZB6emmmb2u0MFMu\F2yeYLpcYllcW5vMT35cH1xcGWweXz9ZYNmfGGvaXTlJIlv[3WkYYTl[EBnd3JiN{KgbJJ{NCCLQ{WwJF0hOC5yMUmg{txONg>?	MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNlE6PDJ{Lze+R4hGVUKOPD;hQi=>
SW1417	MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NYTPbGpCPzJiaILz	NHS1WnFIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBUXzF2MUegZ4VtdHNiYYSgNVoyOCCvb3zhdkBz[XSrbzDv[kBkd22yb4Xu[EBqdiCycnXz[Y5k\SCxZjDOMZs{NVt\|LXP5Z4xweHKxcInsMVUuMDJvZnz1c5JwNTRvaX;kc{1xcGWweXzhcYlvdylvNjy4MYRqdWW2aInsMUAzNDRuNz30dolwgG9vMzy0MFYtPy22ZYTyZYh6\HKxLULIMZB6emmmb2u0MFMu\F2yeYLpcYllcW5vMT35cH1xcGWweXz9ZYNmfGGvaXTlJIlv[3WkYYTl[EBnd3JiN{KgbJJ{NCCLQ{WwJF0hOC5yMzFOwG0v	M4jpTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIzOTl2MkKvK\|5EcEWPQly8M4E,
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RKO	Mn3ES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NH;NSGo4OiCqcoO=	NED4bFVIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBTU09iY3XscJMh[XRiMUqxNEBud2yjcjDyZZRqdyCxZjDjc41xd3WwZDDpckBxemW\|ZX7j[UBw\iCQLYuzMXs{NWO7Y3zvdJJweHmuLUWtLFIu\my3b4LvMVQucW:mbz3wbIVvgWyjbXnuc{kuPix6LXTpcYV1cHmuLTCyMFQtPy22cnnvfI8uOyx2LE[sO{11\XS{YXj5[JJwNTKKLYD5dolld1t2LEOt[H1xgXKrbXnkbY4uOS27bG3wbIVvgWy;YXPleIFucWSnIHnuZ5Vj[XSnZDDmc5IhPzJiaILzMEBKSzVyIE2gNE4xPTRizszNMi=>	MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNlE6PDJ{Lze+R4hGVUKOPD;hQi=>
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NCI-H1155	NYWzWFhMT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NWnmPJZXPzJiaILz	MYTHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDOR2kuUDFzNUWgZ4VtdHNiYYSgNVoyOCCvb3zhdkBz[XSrbzDv[kBkd22yb4Xu[EBqdiCycnXz[Y5k\SCxZjDOMZs{NVt\|LXP5Z4xweHKxcInsMVUuMDJvZnz1c5JwNTRvaX;kc{1xcGWweXzhcYlvdylvNjy4MYRqdWW2aInsMUAzNDRuNz30dolwgG9vMzy0MFYtPy22ZYTyZYh6\HKxLULIMZB6emmmb2u0MFMu\F2yeYLpcYllcW5vMT35cH1xcGWweXz9ZYNmfGGvaXTlJIlv[3WkYYTl[EBnd3JiN{KgbJItKEmFNUCgQUAxNjFyMTFOwG0v	NH3KOHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOjF7NEKyM{c,S2iHTVLMQE9iRg>?
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NCI-H727	NHPSdGNIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	M4PFXVczKGi{cx?=	M4X4S2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KN{K3JINmdGy\|IHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KEOnbHyteIl1\XJvR3zvJJJm[WenboSgZoF{\WRiYYPzZZktKEmFNUCgQUA1Njd7OTFOwG0v	NEfWfYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOjF7NEKyM{c,S2iHTVLMQE9iRg>?
COR-L23	NGTaV41Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NXWwRpdOPzJiaILz	MXXHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDDU3IuVDJ\|IHPlcIx{KGmwY4XiZZRm\CCob4KgO\|IhcHK\|IHL5JGNmdGxvdHn0[ZIuT2yxIILlZYdmdnRiYnHz[YQh[XO\|YYmsJGlEPTBiPTC1MlM4OyEQvF2u	NE\FdYs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOjF7NEKyM{c,S2iHTVLMQE9iRg>?
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NCI-H1355	MortS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MkC5O\|IhcHK\|	Ml3NS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUmNKNUhzM{W1JINmdGy\|IHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KEOnbHyteIl1\XJvR3zvJJJm[WenboSgZoF{\WRiYYPzZZktKEmFNUCgQUA3NjZ6NTFOwG0v	NUexbGVKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjJzOUSyNk8oRkOqRV3CUFww[T5?
NCI-H23	NEThXXBIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	M4jGRVczKGi{cx?=	MVjHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDOR2kuUDJ\|IHPlcIx{KGmwY4XiZZRm\CCob4KgO\|IhcHK\|IHL5JGNmdGxvdHn0[ZIuT2yxIILlZYdmdnRiYnHz[YQh[XO\|YYmsJGlEPTBiPTC3MlEzPCEQvF2u	MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNlE6PDJ{Lze+R4hGVUKOPD;hQi=>
NCI-H1792	NWn3ZWZ5T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MlXSO\|IhcHK\|	MYnHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDOR2kuUDF5OUKgZ4VtdHNiaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhS2WubD30bZRmei2JbH:gdoVi\2WwdDDiZZNm\CCjc4PhfUwhUUN3MDC9JFcvOzB5IN88UU4>	M2Lud\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIzOTl2MkKvK\|5EcEWPQly8M4E,
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... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-GSK3 / GSK3 / p-PRAS40 / PRAS40 / p-FOXO / p-Casp9 / p-AKT / AKT / p-MEK / p-ERK / Erk ; PubMed: 24978597 PLoS One BT474 (left) and LNCaP (right) cell lines were treated with DMSO or GSK2110183 for 1 h. Western analysis was performed to assay levels of phosphorylated and total GSK-3, PRAS40, AKT and ERK, phosphorylated Foxo, Caspase 9, and MEK. Tubulin was used as a loading control. ATG3 / ATG12 / LC3B ; PubMed: 30867818 Theranostics Alterations in autophagy-related proteins induced by AKT inhibition.	24978597 30867818

In vivo

Mice bearing BT474 breast tumor xenografts are dosed with afuresertib (p.o.) at 10, 30 or 100 mg/kg daily which results in 8, 37 and 61% TGI, respectively. Mice bearing SKOV3 ovarian tumor xenografts are treated with 10, 30 and 100 mg/kg afuresertib which results in 23, 37 and 97% TGI, respectively.^[1]

Protocol

Kinase Assay:^[1]	- Collapse Potency (Ki) of afuresertib: The true potency (Ki) of the inhibitor is initially determined at low enzyme concentrations (0.1 nM AKT1, 0.7 nM AKT2, and 0.2 nM AKT3) using a filter binding assay and then confirmed with progress curve analysis. In the filter binding assay, a pre-mix of enzyme plus inhibitor is incubated for 1 h and then added to a GSKα peptide (Ac-KKGGRARTSS-FAEPG-amide) and [γ³³P] ATP. Reactions are terminated after 2 h and the radio labeled AKT peptide product is captured in a phospho-cellulose filter plate. Progress curve analysis utilizes continuous real-time fluorescence detection of product formation using the Sox-AKT-tide substrate (Ac-ARKRERAYSF-d-Pro-Sox-Gly-NH2).
Cell Research:^[1]	- Collapse Cell lines: Hematological cell lines and solid tumor cell lines Concentrations: 30 μM Incubation Time: 72 h Method: A 3-day proliferation assay using CellTiter-Glo is performed to measure the growth inhibition by the compounds at 0-30 μM. Cell growth is determined relative to untreated (DMSO) controls. EC50’s are calculated from inhibition curves using a 4- or 6-parameter fitting algorithm in the Assay Client application. (Only for Reference)
Animal Research:^[1]	- Collapse Animal Models: Female athymic nude and SCID mice bearing SKOV3 or BT474 tumors Dosages: 100 mg/kg Administration: p.o. (Only for Reference)

References

[1] Dumble M, et al. PLoS One, 2014, 9(6):e100880.

Solubility (25°C)

In vitro	DMSO	85 mg/mL (198.91 mM)
	Ethanol	85 mg/mL (198.91 mM)
	Water	Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download Afuresertib (GSK2110183) SDF

Molecular Weight	427.32
Formula	C₁₈H₁₇Cl₂FN₄OS
CAS No.	1047644-62-1
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	CN1C(=C(C=N1)Cl)C2=C(SC(=C2)C(=O)NC(CC3=CC(=CC=C3)F)CN)Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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mg/kg

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Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

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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 addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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The Serial Dilution Calculator Equation

Serial Dilutions
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Computed Result

C1=C0/X	C1:	LOG(C1):
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Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-01-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04374630	Recruiting	Drug: Paclitaxel\|Drug: Afuresertib	Platinum-resistant Ovarian Cancer	Laekna Limited	June 9 2020	Phase 2
NCT04060394	Recruiting	Drug: Phase I and Phase II: LAE001/prednisone + afuresertib	Metastatic Castration-resistant Prostate Cancer	Laekna Limited	September 13 2019	Phase 1\|Phase 2
NCT02235740	Terminated	Drug: Afuresertib\|Drug: Carfilzomib	Cancer	Novartis\|Amgen	November 2014	Phase 1
NCT02240212	Completed	Drug: Afuresertib\|Drug: Paclitaxel	Cancer	Novartis Pharmaceuticals\|Novartis	October 2014	Phase 1
NCT02177682	Terminated	Drug: Afuresertib	Neoplasms Haematologic	Novartis Pharmaceuticals\|Novartis	August 13 2014	Phase 1

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Akt Signaling Pathway Map

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Afuresertib (GSK2110183)