Shanghai Nianxing Industrial Co., Ltd
China
Product Name: Hu7691
Price:
Purity: 99.86%
Stocking Period: 10 Day
Contact: Yang

DC Chemicals Limited
China
Product Name: Hu7691
Price: ￥Inquiry/100mg ￥Inquiry/250mg ￥Inquiry/1g
Purity: 98.0%
Stocking Period: 1 Day
Contact: Tony Cao

2360523-76-6

2360523-76-6 structure

2360523-76-6 structure

Name: Hu7691
Chemical Name: Hu7691
CAS Number: 2360523-76-6
Molecular Formula: C₂₂H₂₂ClF₃N₄O
Molecular Weight: 450.88
Catalog: Signaling Pathways Cell Cycle/DNA Damage ROCK
Create Date: 2021-10-08 18:54:47
Modify Date: 2024-01-11 10:27:51
Hu7691 is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 inhibits tumor growth and enables decrease of cutaneous toxicity in mice[1].

Name	Hu7691

Description	Hu7691 is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 inhibits tumor growth and enables decrease of cutaneous toxicity in mice[1].
Related Catalog	Signaling Pathways >> Epigenetics >> PKC Research Areas >> Cancer Signaling Pathways >> Metabolic Enzyme/Protease >> SGK Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PKA Signaling Pathways >> Stem Cell/Wnt >> PKA Signaling Pathways >> Cell Cycle/DNA Damage >> ROCK Signaling Pathways >> PI3K/Akt/mTOR >> Akt Signaling Pathways >> MAPK/ERK Pathway >> Ribosomal S6 Kinase (RSK) Signaling Pathways >> TGF-beta/Smad >> PKC Signaling Pathways >> Stem Cell/Wnt >> ROCK Signaling Pathways >> TGF-beta/Smad >> ROCK
Target	Akt1:4.0 nM (IC50) Akt2:97.5 nM (IC50) Akt3:28 nM (IC50) PKA:11 nM (IC50) PKCη:629 nM (IC50) ROCK1:354 nM (IC50) RSK1:756 nM (IC50) p70S6K:229 nM (IC50)
In Vitro	Hu7691 displays low inhibitions against most of the kinases in the four families (AGC, TK, TKL, Lipid/Atypical; PKA, IC50=11 nM; PKCη, IC50=629 nM; ROCK1, IC50=354 nM; RSK1, IC50=756 nM; P70S6K, IC50=229 nM; SGK, IC50=1009 nM)[1]. Hu7691 (2.25-36 μM; 24 hours) induces effective decrease of the phosphorylation level of Akt (S473)[1]. B5 (10, 20, 30, 40 μM; for 72 h) exhibits low toxicity against HaCaT cells with an IC50 value of 15.2 μM[1]. Hu7691 has a significant inhibitory effect on the growth of 18 kinds of human tumor cells (U87-MG, U251, A549, HepG2, HT-29, KHOS, MDA-MB-231, PC3, SKOV3 and so on) derived from different tissues, with the IC50 range of 0.6-27 μM. Hu7691 shows low antiproliferation activities against the HL7702 and HPDE6-C7 normal cells, exhibiting IC50 values of 5.4 and 16.1 μM, respectively[1]. Western Blot Analysis[1] Cell Line: HaCaT cells Concentration: 2.25, 4.5, 9, 18, 36 μM Incubation Time: 24 hours Result: Induced effective decrease of the phosphorylation level of Akt (S473).
In Vivo	Hu7691 (12.5-50 mg/kg/day; i.g.; for 22 days) shows dose-dependent tumor growth inhibition[1]. Hu7691 (15 mg/kg; oral) has a T1/2 of 8.68 hours, a Cmax of 171.17 ng/mL and an AUC of 2820.64 ng/mL•h in rats[1]. Hu7691 (2 mg/kg; iv) has a T1/2 of 6.24 hours, a Cmax of 207.52 ng/mL and an AUC of 532.87 ng/mL•h in rats[1]. Hu7691 (20 mg/kg; oral) has a T1/2 of 16.7 hours, a Cmax of 905.65 ng/mL and an AUC of 36303 ng/mL•h in beagle dog (male, 40 weeks old, 8–10 kg)[1]. Animal Model: Balb/c mice (nu/nu, female, 3-4 weeks old, 20-25 g) with 786-O and KHOS xenograft[1] Dosage: 12.5, 25, 50 mg/kg Administration: Oral; once daily for 22 days Result: Showed dose-dependent tumor growth inhibition. Animal Model: SD rats (male, 8 weeks old, 250-300 g)[1] Dosage: 15 mg/kg (Pharmacokinetic Analysis) Administration: Oral Result: Had a T1/2 of 8.68 hours, a Cmax of 171.17 ng/mL and an AUC of 2820.64 ng/mL•h.
References	[1]. Jinxin Che, et al. Discovery of N-((3 S,4 S)-4-(3,4-Difluorophenyl)piperidin-3-yl)-2-fluoro-4-(1-methyl-1 H-pyrazol-5-yl)benzamide (Hu7691), a Potent and Selective Akt Inhibitor That Enables Decrease of Cutaneous Toxicity. J Med Chem. 2021 Aug 26;64(16):12163-12180.

Molecular Formula	C₂₂H₂₂ClF₃N₄O
Molecular Weight	450.88

Hazard Codes	Xi