Product 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.
CAS:
2360523-76-6
Molecular Weight:
450.88
Formula:
C22H22ClF3N4O
Chemical Name:
N-((3S, 4S)-4-(3, 4-difluorophenyl)piperidin-3-yl)-2-fluoro-4-(1-methyl-1H-pyrazol-5-yl)benzamide hydrochloride
Smiles :
Cl.CN1N=CC=C1C1=CC=C(C(=O)N[C@@H]2CNCC[C@H]2C2=CC=C(F)C(F)=C2)C(F)=C1
InChiKey:
WHVFOLXIIVBJTJ-ICCPGPOKSA-N
InChi :
InChI=1S/C22H21F3N4O.ClH/c1-29-21(7-9-27-29)14-2-4-16(18(24)11-14)22(30)28-20-12-26-8-6-15(20)13-3-5-17(23)19(25)10-13;/h2-5,7,9-11,15,20,26H,6,8,12H2,1H3,(H,28,30);1H/t15-,20+;/m0./s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.Domvanalimab medchemexpress
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
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.|Product information|CAS Number: 2360523-76-6|Molecular Weight: 450.88|Formula: C22H22ClF3N4O|Chemical Name: N-((3S, 4S)-4-(3, 4-difluorophenyl)piperidin-3-yl)-2-fluoro-4-(1-methyl-1H-pyrazol-5-yl)benzamide hydrochloride|Smiles: Cl.CN1N=CC=C1C1=CC=C(C(=O)N[C@@H]2CNCC[C@H]2C2=CC=C(F)C(F)=C2)C(F)=C1|InChiKey: WHVFOLXIIVBJTJ-ICCPGPOKSA-N|InChi: InChI=1S/C22H21F3N4O.ClH/c1-29-21(7-9-27-29)14-2-4-16(18(24)11-14)22(30)28-20-12-26-8-6-15(20)13-3-5-17(23)19(25)10-13;/h2-5,7,9-11,15,20,26H,6,8,12H2,1H3,(H,28,30);1H/t15-,20+;/m0./s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|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).Pergolide custom synthesis Hu7691 (2.PMID:32619361 25-36 μM; 24 hours) induces effective decrease of the phosphorylation level of Akt (S473). B5 (10, 20, 30, 40 μM; for 72 h) exhibits low toxicity against HaCaT cells with an IC50 value of 15.2 μM. 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.|In Vivo:|Hu7691 (12.5-50 mg/kg/day; i.g.; for 22 days) shows dose-dependent tumor growth inhibition. 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. 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. 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).|Products are for research use only. Not for human use.|