ATR-IN-8

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

ATR-IN-8 

ATR-IN-8 是一种有效的 ATR 抑制剂。ATR是同源重组修复途径中的关键酶,属于 PIKK 家族。ATR-IN-8具有研究癌症疾病的潜力 (摘自专利 WO2021143821A1,化合物 3)。

ATR-IN-8

ATR-IN-8 Chemical Structure

CAS No. : 2672511-20-3

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生物活性

ATR-IN-8 is a potent inhibitor of ATR. ATR is a key enzyme in the homologous recombination repair pathway and belongs to the PIKK family. ATR-IN-8 has the potential for the research of cancer diseases (extracted from patent WO2021143821A1, compound 3)[1].

分子量

410.49

Formula

C20H22N6O2S

CAS 号

2672511-20-3

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.

参考文献
  • [1]. Li Xin, et al. Thickened heteroaryl derivatives, their preparation methods and their application in medicine. Patent WO2021143821A1.

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FGFR-IN-2

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

FGFR-IN-2 

FGFR-IN-2 (compound 1) 是一种有效的 FGFR 抑制剂,对 FGFR1、FGFR2、FGFR3 和 FGFR4 的 IC50 分别为 7.3 nM、4.3 nM、7.6 nM、11 nM。FGFR-IN-2 具有用于癌症研究的潜力。

FGFR-IN-2

FGFR-IN-2 Chemical Structure

CAS No. : 2665665-09-6

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生物活性

FGFR-IN-2 (compound 1) is a potent FGFR inhibitor with IC50s of 7.3 nM, 4.3 nM, 7.6 nM, 11 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. FGFR-IN-2 has the potential for cancer research[1].

IC50 & Target[1]

FGFR1

7.3 nM (IC50)

FGFR2

4.3 nM (IC50)

FGFR3

7.6 nM (IC50)

FGFR4

11 nM (IC50)

分子量

446.54

Formula

C25H30N6O2

CAS 号

2665665-09-6

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.

参考文献
  • [1]. Don Zhang, et al. Pyridazine and 1,2,4-triazine derivatives as fgfr kinase inhibitors. WO2021146163A1.

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KIF18A-IN-3

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

KIF18A-IN-3 

KIF18A-IN-3 是一种有效的 KIF18A 抑制剂 (IC50=61 nM)。KIF18A-IN-3 能引起明显的有丝分裂停滞,增加肿瘤组织中有丝分裂细胞的数量。KIF18A-IN-3 可用于肿瘤研究。

KIF18A-IN-3

KIF18A-IN-3 Chemical Structure

CAS No. : 2600577-49-7

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生物活性

KIF18A-IN-3 is a potent KIF18A inhibitor (IC50=61 nM). KIF18A-IN-3 causes significant mitotic arrest and increases the number of mitotic cells in tumor tissues. KIF18A-IN-3 can be used for researching cancer[1].

IC50 & Target

IC50: 61 nM (KIF18A)[1]

体内研究
(In Vivo)

KIF18A-IN-3 (compound 24) exhibits a significant and sustained pharmacodynamic response, increasing the number of mitotic cells (pH3 positive cells) in tumor tissues for up to 24 hours[1]. Pharmacokinetic Parameters of KIF18A-IN-3 in female CD-1 mice[1].

IP (100 mg/kg)
Cmax (μM) 26.5
AUC0-24 (μM·h) 269
C24h (μM) 0.8
PPB (fu) 0.015

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female athymic nude mice (4-7 weeks; injected with human OVCAR-3 HGSOC cells)[1]
Dosage: 100 mg/kg
Administration: i.p., single
Result: Showed a significant and sustained pharmacodynamic response, increasing the number of mitotic cells (pH3 positive cells) in tumor tissues for up to 24 hours.

分子量

574.76

Formula

C28H38N4O5S2

CAS 号

2600577-49-7

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.

参考文献
  • [1]. Tamayo NA, et al. Targeting the Mitotic Kinesin KIF18A in Chromosomally Unstable Cancers: Hit Optimization Toward an In Vivo Chemical Probe. J Med Chem. 2022;65(6):4972-4990.

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ER degrader 2

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

ER degrader 2 

ER degrader 2 是一种有效的雌激素受体 (ER) 降解剂。雌激素信号系统在调节细胞生长、分化和凋亡 (apoptosis) 中发挥着重要作用。ER degrader 2 具有研究癌症疾病的潜力 (摘自专利 CN112830919A,化合物 1)。

ER degrader 2

ER degrader 2 Chemical Structure

CAS No. : 2390147-41-6

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生物活性

ER degrader 2 is a potent degrader of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. ER degrader 2 has the potential for the research of cancer diseases (extracted from patent CN112830919A, compound 1)[1].

分子量

625.72

Formula

C34H42F3N5O3

CAS 号

2390147-41-6

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.

参考文献
  • [1]. Miaomiao Zhao, et al. Benzopiperidine derivatives pharmaceutically available salts and methods for their preparation. Patent CN112830919A.

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Estrogen receptor antagonist 3

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Estrogen receptor antagonist 3 

Estrogen receptor antagonist 3 是一种有效的雌激素受体 (ER) 降解剂。雌激素信号系统在调节细胞生长、分化和凋亡 (apoptosis) 中发挥着重要作用。Estrogen receptor antagonist 4 具有研究癌症疾病的潜力 (摘自专利 WO2021213358A1,化合物 7)。

Estrogen receptor antagonist 3

Estrogen receptor antagonist 3 Chemical Structure

CAS No. : 2730011-50-2

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生物活性

Estrogen receptor antagonist 3 is a potent antagonist of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. Estrogen receptor antagonist 3 has the potential for the research of cancer diseases (extracted from patent WO2021213358A1, compound 7)[1].

分子量

554.34

Formula

C26H29BF6N4O2

CAS 号

2730011-50-2

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.

参考文献
  • [1]. Gu Peng, et al. Boron-containing compounds and their applications. Patent WO2021213358A1.

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ER degrader 3

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

ER degrader 3 

ER degrader 3 是一种有效的雌激素受体 (ER) 降解剂。雌激素信号系统在调节细胞生长、分化和凋亡 (apoptosis) 中发挥着重要作用。ER degrader 3 具有研究癌症疾病的潜力 (摘自专利 WO2018233591A1,化合物 1)。

ER degrader 3

ER degrader 3 Chemical Structure

CAS No. : 2254818-47-6

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生物活性

ER degrader 3 is a potent degrader of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. ER degrader 3 has the potential for the research of cancer diseases (extracted from patent WO2018233591A1, compound 1)[1].

分子量

649.82

Formula

C39H47N5O4

CAS 号

2254818-47-6

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.

参考文献
  • [1]. Lingfeng You, et al. A kind of salt of benzopiperidine derivatives, its crystal form and salt, the preparation method of its crystal form. Patent WO2018233591A1.

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CC214-2

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

CC214-2 

CC214-2 是一种有效的 mTORC1/mTORC2 双重抑制剂。结核分枝杆菌调节哺乳动物雷帕霉素靶蛋白 (mTOR) 信号传导以阻止自噬。CC214-2 有可能缩短结核病的持续时间。

CC214-2

CC214-2 Chemical Structure

CAS No. : 1228012-18-7

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生物活性

CC214-2 is a potent and dual inhibitor of mTORC1/mTORC2. Mycobacterium tuberculosis modulates mammalian target of rapamycin (mTOR) signaling to impede autophagy. CC214-2 has the potential to shorten the duration of TB[1].

分子量

383.44

Formula

C20H25N5O3

CAS 号

1228012-18-7

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.

参考文献
  • [1]. Tasneen R, et al. Dual mTORC1/mTORC2 Inhibition as a Host-Directed Therapeutic Target in Pathologically Distinct Mouse Models of Tuberculosis. Antimicrob Agents Chemother. 2021;65(7):e0025321.

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Estrogen receptor antagonist 4

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Estrogen receptor antagonist 4 

Estrogen receptor antagonist 4 是一种有效的雌激素受体 (ER) 降解剂。雌激素信号系统在调节细胞生长、分化和凋亡 (apoptosis) 中发挥着重要作用。Estrogen receptor antagonist 4 具有研究癌症疾病的潜力 (摘自专利 WO2021213358A1,化合物 1)。

Estrogen receptor antagonist 4

Estrogen receptor antagonist 4 Chemical Structure

规格 是否有货
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生物活性

Estrogen receptor antagonist 4 is a potent antagonist of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. Estrogen receptor antagonist 4 has the potential for the research of cancer diseases (extracted from patent WO2021213358A1, compound 1)[1].

分子量

476.34

Formula

C24H32BF3N4O2

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.

参考文献
  • [1]. Gu Peng, et al. Boron-containing compounds and their applications. Patent WO2021213358A1.

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DMUP

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

DMUP 

DMUP 是一种有效的 CD47-SIRPα axis 抑制剂。DMUP 在 A549 细胞中诱导细胞凋亡 (apoptosis) 并增加巨噬细胞的吞噬作用。DMUP 降低 CD47 和 SIRPα 的蛋白表达水平。DMUP 显示出抗肿瘤活性。

DMUP

DMUP Chemical Structure

CAS No. : 2364350-07-0

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生物活性

DMUP is a potent CD47-SIRPα axis inhibitor. DMUP induces apoptosis and increases the macrophage phagocytosis in A549 cells. DMUP decreases the expression of CD47 and SIRPα protein. DMUP shows antitumor activity[1].

体外研究
(In Vitro)

DMUP (72 h) shows antiproliferative activity with IC50s of 0.92, 3.58, 6.29, 1.54 µM for A549, A549/DDP, PANC-1, HepG2 cells, respectively[1].
DMUP (5 µM, 24 h) arrests the cell cycle in S phase in A549 cells[1].
DMUP (5 µM, 48 h) induces apoptosis in A549 cells[1].
DMUP (5 µM, 24 h) decreases the expression of CD47 and SIRPα protein[1].
DMUP (5 µM, 4 h) increases the macrophage phagocytosis in A549-GFP cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: A549, A549/DDP, PANC-1, HepG2 cells
Concentration: 0-64 µM
Incubation Time: 72 h
Result: Showed antiproliferative activity with IC50s of 0.92, 3.58, 6.29, 1.54 µM for A549, A549/DDP, PANC-1, HepG2 cells, respectively.

Cell Cycle Analysis[1]

Cell Line: A549 cells
Concentration: 5 µM
Incubation Time: 24 h
Result: Arrested the cell cycle in the S phase.

Apoptosis Analysis[1]

Cell Line: A549 cells
Concentration: 5 µM
Incubation Time: 48 h
Result: Induced cell apoptosis.

Western Blot Analysis[1]

Cell Line: A549, THP-1 cells
Concentration: 5 µM
Incubation Time: 24 h
Result: Decreased the expression of CD47 and SIRPα protein.

体内研究
(In Vivo)

DMUP (10 mg/kg, i.v., every other day for 17 day) shows antitumor activity[1].
DMUP (5, 10, 20, 40 mg/kg, i.v.,every two days for 18 days) shows no toxicity in mice[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ICR mice[1]
Dosage: 5, 10, 20, 40 mg/kg
Administration: i.v., every two days, 18 days
Result: Showed low toxicity with LD50 of greater than 20 mg/kg.
Animal Model: A549 xenograft BALB/c nude mice[1]
Dosage: 10 mg/kg
Administration: i.v., every other day, 17 day
Result: Showed antitumor activity.

分子量

766.44

Formula

C24H24Cl2N2O10Pt

CAS 号

2364350-07-0

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.

参考文献
  • [1]. Tan Y, et al. Platinum(IV) complexes as inhibitors of CD47-SIRPα axis for chemoimmunotherapy of cancer. Eur J Med Chem. 2022; 229:114047.

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KIF18A-IN-2

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

KIF18A-IN-2 

KIF18A-IN-2 是一种有效的 KIF18A 抑制剂 (IC50=28 nM)。KIF18A-IN-2 能引起明显的有丝分裂停滞,增加肿瘤组织中有丝分裂细胞的数量。KIF18A-IN-2 可用于肿瘤研究。

KIF18A-IN-2

KIF18A-IN-2 Chemical Structure

CAS No. : 2600559-20-2

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生物活性

KIF18A-IN-2 is a potent KIF18A inhibitor (IC50=28 nM). KIF18A-IN-2 causes significant mitotic arrest and increases the number of mitotic cells in tumor tissues. KIF18A-IN-2 can be used for researching cancer[1].

IC50 & Target

IC50: 28 nM (KIF18A)[1]

体内研究
(In Vivo)

KIF18A-IN-2 (compound 23) (100 mg/kg; i.p., single) exhibits a significant and sustained pharmacodynamic response, increasing the number of mitotic cells (pH3 positive cells) in tumor tissues for up to 24 hours[1]. Pharmacokinetic Parameters of KIF18A-IN-2 in female CD-1 mice[1].

IP (100 mg/kg)
Cmax (μM) 12.6
AUC0-24 (μM·h) 147
C24h (μM) 2.9
PPB (fu) 0.007

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female athymic nude mice (4-7 weeks; injected with human OVCAR-3 HGSOC cells)[1]
Dosage: 100 mg/kg
Administration: i.p., single
Result: Showed a significant and sustained pharmacodynamic response, increasing the number of mitotic cells (pH3 positive cells) in tumor tissues for up to 24 hours.

分子量

534.69

Formula

C25H34N4O5S2

CAS 号

2600559-20-2

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.

参考文献
  • [1]. Tamayo NA, et al. Targeting the Mitotic Kinesin KIF18A in Chromosomally Unstable Cancers: Hit Optimization Toward an In Vivo Chemical Probe. J Med Chem. 2022;65(6):4972-4990.

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ATM-IN-1

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

ATM-IN-1 

ATM-IN-1 是一种有效的 ATM 抑制剂。ATM 主要位于细胞核和微粒体中,参与细胞周期进程和细胞周期检查点对 DNA 损伤的反应。ATM-IN-1 具有研究癌症和神经疾病的潜力 (摘自专利 WO2021139814A1,化合物 3)。

ATM-IN-1

ATM-IN-1 Chemical Structure

CAS No. : 2662761-76-2

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生物活性

ATM-IN-1 is a potent inhibitor of ATM. ATM is located mainly in the nucleus and microsomes and is involved in cell cycle progression and in the cell cycle checkpoint response to DNA damage. ATM-IN-1 has the potential for the research of cancer and neurology diseases (extracted from patent WO2021139814A1, compound 3)[1].

分子量

528.65

Formula

C30H36N6O3

CAS 号

2662761-76-2

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.

参考文献
  • [1]. Wenyuan Qian, et al. Quinoline and imidazole compounds and their applications. Patent WO2021139814A1.

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Antitumor agent-51

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Antitumor agent-51 

Antitumor agent-51 对骨肉瘤细胞的生长和迁移具有有效的选择性抑制作用,对 MNNG/HOS 细胞的 IC50 为 21.9 nM。Antitumor agent-51 具有低毒性和相当大的生物利用度。

Antitumor agent-51

Antitumor agent-51 Chemical Structure

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生物活性

Antitumor agent-51 possesses potent and selective inhibitory for osteosarcoma cell growth and migration with IC50 of 21.9 nM in MNNG/HOS cells. Antitumor agent-51 has a considerable bioavailability and a low toxicity[1].

IC50 & Target

IC50: 21.9 nM in MNNG/HOS cells[1]

体外研究
(In Vitro)

Antitumor agent-51 (compound R-8i) (0-20 μM; 72 hours) selectively inhibits MNNG/HOS OS cells proliferation with IC50=21.9 nM, and has much less inhibitory activity on two normal BMSC and GES1 cells (IC50>10 μM)[1].
Antitumor agent-51 (5 nM; 24 hours) induces a cell cycle arrest in MNNG/HOS cells with a 23% increase in G0/G1 phase, but no apparent cell apoptosis[1].
Antitumor agent-51 (5 and 20 nM; 24 hours) significantly suppresses the migration of MNNG/HOS cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: MNNG/HOS, MG63, SJSA-1, U2OS, 143B, SAOS-2, HOS, SW1353, GES1, and BMSC cells[1]
Concentration: 0-20 μM
Incubation Time: 72 hours
Result: Selectively inhibited MNNG/HOS cells proliferation with IC50=21.9 nM, and showed much less inhibitory activity on two normal BMSC and GES1 cells (IC50>10 μM).

Cell Cycle Analysis

Cell Line: MNNG/HOS cells[1]
Concentration: 5 nM
Incubation Time: 24 hours
Result: Induced a cell cycle arrest with a 23% increase in G0/G1 phase, but no apparent cell apoptosis.

体内研究
(In Vivo)

Antitumor agent-51 (12.5 or 62.5 mg/kg; i.p. or i.v., single) exhibits good intraperitoneal plasma exposures (AUC0-∞>6900 h ng/mL) and an acceptable bioavailability (52.1%) for the i.p. administration in male ICR mice[1].
Antitumor agent-51 (62.5 mg/kg; i.p., twice per day for 18 days) significantly suppresses MNNG/HOS tumor growth with tumor growth inhibition (TGI) of 52.9% and does not induce an obvious toxicity in nude mice[1].
Pharmacokinetic Parameters of Antitumor agent-51 in male ICR mice[1].

IV (12.5 mg/kg) IP (62.5 mg/kg)
T1/2 (h) 0.061 0.641
AUC0-inf (h·ng/mL) 3230 8406
Cmax (ng/mL) 20511
CL (mL/min/kg) 66.9
F (%) 52.1

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male ICR mice (30 g, n=3)[1]
Dosage: 12.5 or 62.5 mg/kg
Administration: i.p. or i.v., single (Pharmacokinetic Analysis)
Result: Showed good intraperitoneal plasma exposures (AUC0-∞ > 6900 h ng/mL) and an acceptable bioavailability (52.1%) for the i.p. administration.
Animal Model: Female BALB/c nude mice (3 months, human MNNG/HOS xenografts)[1]
Dosage: 62.5 mg/kg
Administration: i.p., twice per day for 18 days
Result: Significantly suppressed MNNG/HOS tumor growth with tumor growth inhibition (TGI) of 52.9% and did not induce an obvious toxicity.

分子量

435.54

Formula

C23H25N5O2S

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.

参考文献
  • [1]. Deng Y, et al. Novel 2-phenyl-3-(Pyridin-2-yl) thiazolidin-4-one derivatives as potent inhibitors for proliferation of osteosarcoma cells in vitro and in vivo. Eur J Med Chem. 2022;228:114010.

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FGFR-IN-2

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

FGFR-IN-2 

FGFR-IN-2 (compound 1) 是一种有效的 FGFR 抑制剂,对 FGFR1、FGFR2、FGFR3 和 FGFR4 的 IC50 分别为 7.3 nM、4.3 nM、7.6 nM、11 nM。FGFR-IN-2 具有用于癌症研究的潜力。

FGFR-IN-2

FGFR-IN-2 Chemical Structure

CAS No. : 2665665-09-6

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生物活性

FGFR-IN-2 (compound 1) is a potent FGFR inhibitor with IC50s of 7.3 nM, 4.3 nM, 7.6 nM, 11 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. FGFR-IN-2 has the potential for cancer research[1].

IC50 & Target[1]

FGFR1

7.3 nM (IC50)

FGFR2

4.3 nM (IC50)

FGFR3

7.6 nM (IC50)

FGFR4

11 nM (IC50)

分子量

446.54

Formula

C25H30N6O2

CAS 号

2665665-09-6

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.

参考文献
  • [1]. Don Zhang, et al. Pyridazine and 1,2,4-triazine derivatives as fgfr kinase inhibitors. WO2021146163A1.

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KIF18A-IN-4

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

KIF18A-IN-4 

KIF18A-IN-4 是一种中度有效的 ATP 和微管 (microtubule) 非竞争性 KIF18A 抑制剂 (IC50=6.16 μM)。KIF18A-IN-4 对大量有丝分裂驱动蛋白和激酶具有选择性,对微管蛋白组装没有任何直接影响。具有抗肿瘤活性。

KIF18A-IN-4

KIF18A-IN-4 Chemical Structure

CAS No. : 1197522-21-6

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生物活性

KIF18A-IN-4 is a moderately potent ATP and microtubule (MT) noncompetitive KIF18A inhibitor (IC50=6.16 μM). KIF18A-IN-4 has selectivity against a large panel of mitotic kinesins and kinases, and does not show any direct effects on tubulin assembly. KIF18A-IN-4 exhibits anti-tumor activity[1].

IC50 & Target

IC50: 6.16 μM (KIF18A)[1]

体外研究
(In Vitro)

KIF18A-IN-4 (15 μM; 24 hours) induces a phenotype characterized by multipolar spindle arrays emanating from multiple pericentriolar material (PCM) centers in mitotic MDA-MB-157 cells (pH3+)[1].
KIF18A-IN-4 (0-10 μM; overnight) has an EC50 of 6.35 μM in OVCAR-3 cells by the mitotic index assay[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

413.53

Formula

C22H27N3O3S

CAS 号

1197522-21-6

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.

参考文献
  • [1]. Tamayo NA, et al. Targeting the Mitotic Kinesin KIF18A in Chromosomally Unstable Cancers: Hit Optimization Toward an In Vivo Chemical Probe. J Med Chem. 2022;65(6):4972-4990.

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ER degrader 1

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

ER degrader 1 

ER degrader 1 是一种有效的雌激素受体 (ER) 降解剂。雌激素信号系统在调节细胞生长、分化和凋亡 (apoptosis) 中发挥着重要作用。ER degrader 1 具有研究癌症疾病的潜力 (摘自专利 WO2021139756A1,化合物 11)。

ER degrader 1

ER degrader 1 Chemical Structure

CAS No. : 2667015-33-8

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生物活性

ER degrader 1 is a potent degrader of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. ER degrader 1 has the potential for the research of cancer diseases (extracted from patent WO2021139756A1, compound 11)[1].

分子量

524.55

Formula

C26H32F4N4O3

CAS 号

2667015-33-8

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.

参考文献
  • [1]. Fanglong Yang, et al. Tricyclic tetrahydroisoquinoline derivatives, their preparation methods and their application in medicine. Patent WO2021139756A1.

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Estrogen receptor antagonist 3

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Estrogen receptor antagonist 3 

Estrogen receptor antagonist 3 是一种有效的雌激素受体 (ER) 降解剂。雌激素信号系统在调节细胞生长、分化和凋亡 (apoptosis) 中发挥着重要作用。Estrogen receptor antagonist 4 具有研究癌症疾病的潜力 (摘自专利 WO2021213358A1,化合物 7)。

Estrogen receptor antagonist 3

Estrogen receptor antagonist 3 Chemical Structure

CAS No. : 2730011-50-2

规格 是否有货
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生物活性

Estrogen receptor antagonist 3 is a potent antagonist of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. Estrogen receptor antagonist 3 has the potential for the research of cancer diseases (extracted from patent WO2021213358A1, compound 7)[1].

分子量

554.34

Formula

C26H29BF6N4O2

CAS 号

2730011-50-2

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.

参考文献
  • [1]. Gu Peng, et al. Boron-containing compounds and their applications. Patent WO2021213358A1.

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ATR-IN-8

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

ATR-IN-8 

ATR-IN-8 是一种有效的 ATR 抑制剂。ATR是同源重组修复途径中的关键酶,属于 PIKK 家族。ATR-IN-8具有研究癌症疾病的潜力 (摘自专利 WO2021143821A1,化合物 3)。

ATR-IN-8

ATR-IN-8 Chemical Structure

CAS No. : 2672511-20-3

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生物活性

ATR-IN-8 is a potent inhibitor of ATR. ATR is a key enzyme in the homologous recombination repair pathway and belongs to the PIKK family. ATR-IN-8 has the potential for the research of cancer diseases (extracted from patent WO2021143821A1, compound 3)[1].

分子量

410.49

Formula

C20H22N6O2S

CAS 号

2672511-20-3

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.

参考文献
  • [1]. Li Xin, et al. Thickened heteroaryl derivatives, their preparation methods and their application in medicine. Patent WO2021143821A1.

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AKT-IN-8

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

AKT-IN-8 

AKT-IN-8 是一种有效的 AKT 抑制剂,对 AKT1、AKT2 和 AKT3 的IC50 分别为 4.46、2.44 和 9.47 nM。

AKT-IN-8

AKT-IN-8 Chemical Structure

CAS No. : 2654026-13-6

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生物活性

AKT-IN-8 is a potent AKT inhibitor with IC50s of 4.46, 2.44, and 9.47 nM for AKT1, AKT2, and AKT3, respectively[1].

IC50 & Target[1]

Akt1

4.46 nM (IC50)

Akt2

2.44 nM (IC50)

Akt3

9.47 nM (IC50)

分子量

456.93

Formula

C22H25ClN6O3

CAS 号

2654026-13-6

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.

参考文献
  • [1]. Fused tetracyclic derivative, preparation method therefor, and medical use thereof. WO2021121276A1.

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Estrogen receptor antagonist 4

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Estrogen receptor antagonist 4 

Estrogen receptor antagonist 4 是一种有效的雌激素受体 (ER) 降解剂。雌激素信号系统在调节细胞生长、分化和凋亡 (apoptosis) 中发挥着重要作用。Estrogen receptor antagonist 4 具有研究癌症疾病的潜力 (摘自专利 WO2021213358A1,化合物 1)。

Estrogen receptor antagonist 4

Estrogen receptor antagonist 4 Chemical Structure

规格 是否有货
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生物活性

Estrogen receptor antagonist 4 is a potent antagonist of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. Estrogen receptor antagonist 4 has the potential for the research of cancer diseases (extracted from patent WO2021213358A1, compound 1)[1].

分子量

476.34

Formula

C24H32BF3N4O2

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.

参考文献
  • [1]. Gu Peng, et al. Boron-containing compounds and their applications. Patent WO2021213358A1.

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ER degrader 2

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

ER degrader 2 

ER degrader 2 是一种有效的雌激素受体 (ER) 降解剂。雌激素信号系统在调节细胞生长、分化和凋亡 (apoptosis) 中发挥着重要作用。ER degrader 2 具有研究癌症疾病的潜力 (摘自专利 CN112830919A,化合物 1)。

ER degrader 2

ER degrader 2 Chemical Structure

CAS No. : 2390147-41-6

规格 是否有货
100 mg   询价  
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生物活性

ER degrader 2 is a potent degrader of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. ER degrader 2 has the potential for the research of cancer diseases (extracted from patent CN112830919A, compound 1)[1].

分子量

625.72

Formula

C34H42F3N5O3

CAS 号

2390147-41-6

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.

参考文献
  • [1]. Miaomiao Zhao, et al. Benzopiperidine derivatives pharmaceutically available salts and methods for their preparation. Patent CN112830919A.

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