Hu7691

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摩尔计算器

Hu7691 是一种具有口服活性的，选择性 Akt 抑制剂，对 Akt1、Akt2 和 Akt3 的 IC₅₀ 分别为 4.0 nM、97.5 nM、28 nM。Hu7691 抑制肿瘤生长并降低小鼠的皮肤毒性。

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Hu7691 Chemical Structure

CAS No. : 2360523-76-6

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规格	价格	是否有货
1 mg	￥4000	7 - 9 周
5 mg	现货	7 - 9 周
10 mg	现货	7 - 9 周
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Akt Akt1 Akt2 Akt3

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PKA PKAR

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PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKCι

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ROCK ROCK1 ROCK2

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p70S6K RSK1 RSK2 RSK3 RSK4

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SGK1 SGK3

生物活性
纯度 & 产品资料
参考文献

生物活性

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].

IC₅₀ & Target^[1]

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)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
769-P	IC₅₀	7.76 μM Compound: B5; Hu7691	Antiproliferative activity against human 769-P cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human 769-P cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
786-0	IC₅₀	2.5 μM Compound: B5; Hu7691	Antiproliferative activity against human 786-0 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human 786-0 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 34375113]
786-0	IC₅₀	8.6 μM Compound: B5; Hu7691	Antiproliferative activity against human 786-0 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human 786-0 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
A549	IC₅₀	6.56 μM Compound: B5; Hu7691	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
Bel-7402	IC₅₀	26.62 μM Compound: B5; Hu7691	Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
HaCaT	IC₅₀	15.17 μM Compound: B5; Hu7691	Antiproliferative activity against human HaCaT cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human HaCaT cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 34375113]
HepG2	IC₅₀	3.6 μM Compound: B5; Hu7691	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
HGC-27	IC₅₀	0.68 μM Compound: B5; Hu7691	Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 34375113]
HT-29	IC₅₀	20.29 μM Compound: B5; Hu7691	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
KHOS/NP	IC₅₀	14.86 μM Compound: B5; Hu7691	Antiproliferative activity against human KHOS cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human KHOS cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 34375113]
KHOS/NP	IC₅₀	7.47 μM Compound: B5; Hu7691	Antiproliferative activity against human KHOS cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human KHOS cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
L02	IC₅₀	5.4 μM Compound: B5; Hu7691	Antiproliferative activity against human HL7702 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human HL7702 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
LNCaP	IC₅₀	0.61 μM Compound: B5; Hu7691	Antiproliferative activity against human LNCaP cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human LNCaP cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
MDA-MB-231	IC₅₀	16.37 μM Compound: B5; Hu7691	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
NCI-H1975	IC₅₀	7.56 μM Compound: B5; Hu7691	Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
OS-RC-2	IC₅₀	9.9 μM Compound: B5; Hu7691	Antiproliferative activity against human OS-RC-2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human OS-RC-2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
OVCAR-8	IC₅₀	3.52 μM Compound: B5; Hu7691	Antiproliferative activity against human OVCAR-8 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human OVCAR-8 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
PC-3	IC₅₀	8.74 μM Compound: B5; Hu7691	Antiproliferative activity against human PC3 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human PC3 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
SK-OV-3	IC₅₀	4.71 μM Compound: B5; Hu7691	Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
SMMC-7721	IC₅₀	19.76 μM Compound: B5; Hu7691	Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
U-251	IC₅₀	6.53 μM Compound: B5; Hu7691	Antiproliferative activity against human U251 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human U251 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
U-87MG ATCC	IC₅₀	9.26 μM Compound: B5; Hu7691	Antiproliferative activity against human U-87MG cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human U-87MG cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]

体外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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).

体内研究
(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 T_1/2 of 8.68 hours, a C_max of 171.17 ng/mL and an AUC of 2820.64 ng/mL•h in rats^[1].
Hu7691 (2 mg/kg; iv) has a T_1/2 of 6.24 hours, a C_max of 207.52 ng/mL and an AUC of 532.87 ng/mL•h in rats^[1].
Hu7691 (20 mg/kg; oral) has a T_1/2 of 16.7 hours, a C_max of 905.65 ng/mL and an AUC of 36303 ng/mL•h in beagle dog (male, 40 weeks old, 8–10 kg)^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 T_1/2 of 8.68 hours, a C_max of 171.17 ng/mL and an AUC of 2820.64 ng/mL•h.

分子量

450.88

Formula

C₂₂H₂₂ClF₃N₄O

CAS 号

2360523-76-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料

产品使用指南 (1538 KB)

参考文献

[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):1 [Content Brief]

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摩尔计算器
稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量		浓度		体积		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)	×	体积 _(start)	=	浓度 _(final)	×	体积 _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Hu7691

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