产品名称

英文名称：GDC-0068

同义词

RG7440、GDC0068、GDC 0068、RG-7440、RG 7440、DTXSID9041152、Ipatasertib; GDC-0068、NCGC00182063-03、AS-17027、0RF、IPATASERTIB [WHO-DD]、(2S)-2-(4-chlorophenyl)-1-[4-[(5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]piperazin-1-yl]-3-(propan-2-y、帕他色替

产品性质

CAS编号：1001264-89-6

分子式：C24H32ClN5O2

分子量：458

PubChem编号：24788740

别名：帕他色替

英文别名：RG7440|GDC0068|GDC 0068|RG-7440|RG 7440|DTXSID9041152|Ipatasertib; GDC-0068|NCGC00182063-03|AS-17027|0RF|IPATASERTIB [WHO-DD]|(2S)-2-(4-chlorophenyl)-1-[4-[(5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]piperazin-1-yl]-3-(propan-2-y

规格或纯度：≥98%

英文名称：GDC-0068

生化机理：GDC-0068 is a novel, highly selective oral ATP-competitive inhibitor designed to bind to the 3 isoforms of Akt. GDC-0068 is a highly selective pan-Akt inhibitor targeting Akt1, Akt2 and Akt3 with IC50 of 5 nM, 18 nM and 8 nM, respectively. GDC-0068 inhibits the growth and proliferation of cancer cell lines and xenograft models, including those with loss of PTEN function, oncogenic mutations in PIK3CA, and amplification of HER2. Phase I study of GDC-0068 in patients with refractory solid tumors is ongoing.Selective Akt1/2/3 inhibitor (IC 50 = 5 nM, 18 nM and\xa0 8 nM, respectively). Selective for Akt over PKA (620-fold). ATP-competitive. Antitumor activity in vitro and in vivo .

储存温度：-20°C储存,充氩

运输条件：超低温冰袋运输

备注：有关更多信息，请参阅SDS。有关溶解度，用法和处理的更多建议？请访问我们的常见问题（FAQ）页面以获取更多详细信息。

产品介绍：GDC-0068(RG 7440)是泛Akt抑制剂，对Akt1/2/3的IC50分别为5 nM/18 nM/8 nM，比对PKA的抑制性高620倍。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.

ALogP：2.5

IUPAC Name：(2S)-2-(4-chlorophenyl)-1-[4-[(5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]piperazin-1-yl]-3-(propan-2-ylamino)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

InChi Key：GRZXWCHAXNAUHY-NSISKUIASA-N

Canonical SMILES：CC1CC(C2=C1C(=NC=N2)N3CCN(CC3)C(=O)C(CNC(C)C)C4=CC=C(C=C4)Cl)O

Isomeric SMILES：C[C@@H]1C[C@H](C2=C1C(=NC=N2)N3CCN(CC3)C(=O)[C@H](CNC(C)C)C4=CC=C(C=C4)Cl)O

PubChem CID：24788740

CAS Registry No.：1001264-89-6

ChEMBL Ligand：CHEMBL2177390

RCSB PDB Ligand：0RF

溶解性：DMSO 92 mg/mL Water <1 mg/mL Ethanol 92 mg/mL

敏感性：对湿度敏感

产品包装