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1001264-89-6 (GDC-0068)

1

Identification

GDC-0068 GDC-0068
Name GDC-0068
Formula C24H32ClN5O2
MW 458.0
CAS No. 1001264-89-6
EINECS
Smiles ClC1=CC=C([[email protected]@H](CNC(C)C)C(N2CCN(C3=C([[email protected]](C)C[[email protected]]4O)C4=NC=N3)CC2)=O)C=C1
Synonyms RG7440;GDC0068;GDC 0068;RG-7440;;RG 7440; (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one
InChI InChI=1S/C24H32ClN5O2/c1-15(2)26-13-19(17-4-6-18(25)7-5-17)24(32)30-10-8-29(9-11-30)23-21-16(3)12-20(31)22(21)27-14-28-23/h4-7,14-16,19-20,26,31H,8-13H2,1-3H3/t16-,19-,20-/m1/s1
2

Introduction

GDC-0068(RG 7440) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM, 620-fold selectivity over PKA. IC50 value: 5 nM/18 nM/8 nM(Akt1/2/3) [1] Target: Akt1/2/3 in vitro: Testing against a broad panel of 230 kinases, GDC-0068 only inhibits 3 kinases by >70% at 1 μM concentration (PRKG1α, PRKG1β, and p70S6K, with IC50 of 98 nM, 69 nM, and 860 nM, respectively).

Background Information

A potent APT-competitive and orally available small molecule pan-Akt inhibitor ......by AOBIOUS INC
Ipatasertib, also known as GDC-0068 is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor GDC-0068 binds to and inhibits the activity of Akt in a non-ATP-com ......by BOC Sciences
GDC-0068 is a highly selective pan-Akt inhibitor targeting Akt1/Akt2/Akt3 with IC50 of 5/18/8 nM, 620-fold selectivity over PKA. ......by MedChemexpress Co., Ltd.
GDC-0068 is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor GDC-0068 binds to and inhibits the activity of Akt in a non-ATP-competitive manner, which may result in the inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus). Shelf life: >2 years if stored properly Drug formulation: ......by MedKoo Biosciences, Inc.
Ipatasertib (GDC-0068) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM in cell-free assays, 620-fold selectivity over PKA. Phase 2. ......by Selleck Chemicals LLC
Ipatasertib (GDC-0068) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM, 620-fold selectivity over PKA. Phase 2. ......by Target Molecule Corp.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

Animal Models Female nude mice bearing LNCaP, PC3, KPL-4, or MCF7 tumor xenografts
Dosage ~100 mg/kg/day
Formulation Formulated in 0.5% methylcellulose/0.2% Tween-80
Administration Orally
Source Selleck Chemicals LLC
4

Physical and Chemical Properties

Appearance:White to off-white solid EBNumber:EB000022598

Storage condition

Solubility

DMSO > 80 mg/mL Ethanol > 80 mg/mL by MedChemexpress Co., Ltd.
(25°C) * In vitro DMSO 92 mg/mL (200.87 mM); Ethanol92 mg/mL (200.87 mM); Water<1 mg/mL (<1 mM) by Selleck Chemicals LLC
5

Mechanism and Indication

6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
GDC-0068 Genentech Inc; PPD Development (S) Pte Ltd Metastatic stomach cancer 2013/8/31 2015/8/31 Phase 2 Clinical
GDC-0068 Genentech Inc Hormone refractory prostate cancer 2011/12/31 2016/1/31 Phase 2 Clinical
GDC-0068 Genentech Inc Advanced solid tumor 2012/4/30 2014/8/31 Phase 1 Clinical
GDC-0068 Genentech Inc Advanced solid tumor 2011/7/31 2013/3/31 Phase 1 Clinical
GDC-0068 Genentech Inc Solid tumor 2010/3/31 2013/1/31 Phase 1 Clinical
GDC-0068 - Phase 3
7

Safety Data of GDC-0068

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AOBIOUS INC 1mg/USD21() USA
AbMole BioScience 10mg/USD180(In stock) USA
Active Biochem 5mg/USD110() USA
Aladdin 5mg/RMB3333();50mg/RMB13212() China
Apexbio Technology LLC 5mg/USD100(In stock) USA
BOC Sciences
BioVision, Inc., 1mg/USD95() USA
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD108();10mg/USD144() USA
Cayman Chemical Company 1mg/USD45() USA
DC Chemicals 100mg/USD550(In stock) China
KareBay Biochem 5mg/USD110() USA
MedChemexpress Co., Ltd. 5mg/USD108();10mg/USD144() USA
MedKoo Biosciences, Inc. 10mg/USD120() USA
Novelty (KunShan) Chemical Co., Ltd. China
Selleck Chemicals LLC 5mg/USD270(In stock);10mg/USD370(In stock);10mM/1mLIn DMSO/USD378(In stock);10mM(in 1mL DMSO)/USD476(in 1mL DMSO);50mg/USD1070(In stock);100mg/USD1670(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD108();10mg/USD144() China
Shanghai XingMo Biotechnology Co., Ltd. 1g/USD1200(In stock) CHINA
Target Molecule Corp. 2mg/USD50();5mg/USD98();10mg/USD165();25mg/USD316();50mg/USD540() USA
Thompson Biological Technology Co., Ltd. China
Toronto Research Chemicals Inc. 5mg/USD250() Canada
10

Related Products

Other Forms of 1001264-89-6

Name CAS No Formula MW
GDC-0068 (dihydrochloride) 1396257-94-5 C24H34Cl3N5O2 530.918
GDC-0068 (hydrochloride) 1489263-16-2 C24H33Cl2N5O2 494.46

Recommended Compounds in Akt

Name CAS No Formula MW
3CAI 28755-03-5 C10H8ClNO 193.63
Scutellarin 27740-01-8 C21H18O12 462.36
GSK2110183 1047634-63-8 C18H16Cl2F2N4OS 445.31
GSK2141795 (hydrochloride) 1047635-80-2 C18H17Cl3F2N4O2 465.71
GSK2141795 1047634-65-0 C18H16Cl2F2N4O2 429.25
SB 203580 (hydrochloride) 869185-85-3 C21H17ClFN3OS 413.9
Pachymic acid 29070-92-6 C33H52O5 528.76
Afuresertib (hydrochloride) 1047645-82-8 C18H18Cl3FN4OS 463.78
Afuresertib 1047644-62-1 C18H17Cl2FN4OS 427.32
TIC10 isomer 41276-02-2 C24H26N4O 386.4894
nandrolone decanoate 360-70-3 C28H44O3 428.65
Miltefosine 58066-85-6 C21H46NO4P 407.57
GDC-0068 (dihydrochloride) 1396257-94-5 C24H34Cl3N5O2 530.918
Honokiol 35354-74-6 C18H18O2 266.33
AT7867 (dihydrochloride) 1431697-86-7 C20H22Cl3N3 410.77
Deguelin 522-17-8 C23H22O6 394.42
Triciribine 35943-35-2 C13H16N6O4 320.3
AZD5363 1143532-39-1 C21H25ClN6O2 428.92
AT13148 1056901-62-2 C17H16ClN3O 313.78
Akt1 and Akt2-IN-1 893422-47-4 C33H29N7O 539.6296

Recommended Compounds in Same Indication

Name CAS No Formula MW
AZD1152 722543-31-9 C26H31FN7O6P 587.54
OSI-930 728033-96-3 C22H16F3N3O2S 443.44
TAK-700 (R-form) 752243-39-3 C18H17N3O2 307.35
Olaparib 763113-22-0 C24H23FN4O3 434.46
AT7867 857531-00-1 C20H20ClN3 337.85
NVP-BGJ398 872511-34-7 C26H31Cl2N7O3 560.48
PU-H71 873436-91-0 C18H21IN6O2S 512.37
BMS-599626 (Hydrochloride) 873837-23-1 C27H28ClFN8O3 567.01
RO4987655 874101-00-5 C20H19F3IN3O5 565.28
MGCD-265 analog 875337-44-3 C26H20FN5O2S2 517.5977
Regorafenib (Hydrochloride) 835621-07-3 C21H16Cl2F4N4O3 519.28
AT9283 896466-04-9 C19H23N7O2 381.43
KX2-391 897016-82-9 C26H29N3O3 431.53
Bicalutamide 90357-06-5 C18H14F4N2O4S 430.37
MLN4924 905579-51-3 C21H25N5O4S 443.52
SNX-2112 908112-43-6 C23H27F3N4O3 464.48
Enzalutamide 915087-33-1 C21H16F4N4O2S 464.44
ABC294640 915385-81-8 C23H25ClN2O 380.91
OTSSP167 1431697-89-0 C25H28Cl2N4O2 487.42
MK-0752 471905-41-6 C21H21ClF2O4S 442.9
11

Route of Synthesis

12

References

13

More Information

GDC-0068

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