KRAS G12D inhibitor 12

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。

KRAS G12D inhibitor 12 

KRAS G12D inhibitor 12 是一种有效的 KRAS G12D 抑制剂。Ras 蛋白家族是一种重要的细胞内信号分子,在生长发育中起重要作用。KRAS G12D inhibitor 12 具有研究 KRAS G12D 介导的癌症的潜力 (摘自专利 WO2021108683A1,化合物 134)。

KRAS G12D inhibitor 12

KRAS G12D inhibitor 12 Chemical Structure

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生物活性

KRAS G12D inhibitor 12 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 12 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 134)[1].

分子量

469.90

Formula

C23H21ClFN5O3

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]. Jennifer PITZEN, et al. Covalent ras inhibitors and uses thereof. Patent WO2021108683A1.

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TNIK-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。

TNIK-IN-4 

TNIK-IN-4 是一种有效的 TNIK 抑制剂,IC50 为 0.61 μM。TNIK-IN-4 对典型的结直肠癌细胞系 HCT116 具有抑制活性。

TNIK-IN-4

TNIK-IN-4 Chemical Structure

CAS No. : 2754266-04-9

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生物活性

TNIK-IN-4 is a potent TNIK inhibitor with IC50 of 0.61 μM. TNIK-IN-4 has inhibitory activity against typical colorectal cancer cell line HCT116[1].

IC50 & Target

IC50: 0.61 μM (TNIK)[1]

体外研究
(In Vitro)

TNIK-IN-4 (compound 5a) (0.4-100 μM; 72 hours) has inhibitory activity against typical colorectal cancer cell line HCT116 with IC50 of 36.423 μM[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: HCT116 cells[1]
Concentration: 0.4, 1.2, 3.7, 11.1, 33.3 and 100 μM
Incubation Time: 72 hours
Result: Showed inhibitory activity against typical colorectal cancer cell line HCT116 with IC50 of 36.423 μM.

分子量

365.36

Formula

C20H16FN3O3

CAS 号

2754266-04-9

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]. Luo X, Yang R, Li Y, Zhang L, Yang S, Li L. Discovery of benzo[d]oxazol-2(3H)-one derivatives as a new class of TNIK inhibitors for the treatment of colorectal cancer. Bioorg Med Chem Lett. 2022;67:128745.

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KRAS G12D inhibitor 9

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。

KRAS G12D inhibitor 9 

KRAS G12D inhibitor 9 是一种有效的 KRAS G12D 抑制剂。Ras 蛋白家族是一种重要的细胞内信号分子,在生长发育中起重要作用。KRAS G12D inhibitor 9 具有研究 KRAS G12D 介导的癌症的潜力 (摘自专利 WO2021108683A1,化合物 20)。

KRAS G12D inhibitor 9

KRAS G12D inhibitor 9 Chemical Structure

CAS No. : 2648551-39-5

规格 是否有货
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250 mg   询价  
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生物活性

KRAS G12D inhibitor 9 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 9 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 20)[1].

分子量

569.74

Formula

C33H43N7O2

CAS 号

2648551-39-5

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]. Jennifer PITZEN, et al. Covalent ras inhibitors and uses thereof. Patent WO2021108683A1.

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EGFR-IN-48

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。

EGFR-IN-48 

EGFR-IN-48 是一种有效的且具有口服活性的 EGFR 抑制剂,对 EGFRd19/TM/CS, EGFRLR/TM/CS, EGFRWTIC50 值分别为 0.193 nM, 0.251 nM, 10.4 nM。EGFR-IN-48 抑制 BaF3EGFR del19/T790M/C797S 和 PC-9EGFR del19/T790M/C797S 细胞的增殖,IC50 值分别为 1.526 nM 和 66.7 nM。

EGFR-IN-48

EGFR-IN-48 Chemical Structure

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生物活性

EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC50s of 0.193 nM, 0.251 nM, 10.4 nM for EGFRd19/TM/CS, EGFRLR/TM/CS, EGFRWT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively[1].

IC50 & Target

EGFRd19/TM/CS

0.193 nM (IC50)

EGFRLR/TM/CS

0.251 nM (IC50)

EGFRWT

10.4 nM (IC50)

体外研究
(In Vitro)

EGFR-IN-48 (compound 23) (10 nM) shows anti-proliferative activities against BaF3EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively[1].
EGFR-IN-48 exhibits potent inhibitory activities against various clinically relevant EGFR mutants with IC50s of 10.4, 3.1, 0.9, 0.1, 0.2, 0.3, 0.2 nM for EGFRWT, EGFRLR, EGFRdel19, EGFRdel19/TM, EGFRLR/TM, EGFRLR/TM/CS, EGFRdrl19/TM/CS, respectively[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: BaF3EGFR del19/T790M/C797S, PC-9EGFR del19/T790M/C797S cells
Concentration: 10 nM
Incubation Time:
Result: Showed anti-proliferative activities against BaF3EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively.

体内研究
(In Vivo)

EGFR-IN-48 (2 mg/kg for i.v.; 10 mg/kg for o.p.) shows good oral bioavailability and high plasma exposure in CD-1 mouse[1]. Pharmacokinetic Parameters of EGFR-IN-48 in CD-1 mouse[1].

Route Dose (mg/kg) Vdss (L/kg) T1/2 (h) CL (L/h/kg) AUC0-last (h*ng/mL) Cmax (ng/mL) Tmax (h) F (%)
i.v. 2 0.7 3.3 2.4 13820.0
p.o. 10 33811.0 6600.0 0.5 48.9

CD-1 mouse; 2 mg/kg for i.v.; 10 mg/kg for o.p.[1].

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

Animal Model: CD-1 mouse[1]
Dosage:
Administration: 2 mg/kg for i.v.; 10 mg/kg for o.p.
Result: Showed good oral bioavailability and high plasma exposure.

分子量

800.75

Formula

C35H47BrN9O4PS

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]. Fang H, et al. Design, synthesis and evaluation of the Brigatinib analogues as potent inhibitors against tertiary EGFR mutants (EGFRdel19/T790M/C797S and EGFRL858R/T790M/C797S). Bioorg Med Chem Lett. 2022; 9:128729.

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Tegafur-Uracil(Synonyms: UFT; BMS-200604)

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。

Tegafur-Uracil (Synonyms: UFT; BMS-200604)

Tegafur-Uracil 是一种口服有效的氟尿嘧啶类抗癌剂。Tegafur-Uracil 抑制胸苷酸合成酶。Tegafur-Uracil 可用于抗实体肿瘤研究。

Tegafur-Uracil(Synonyms: UFT;  BMS-200604)

Tegafur-Uracil Chemical Structure

CAS No. : 74578-38-4

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生物活性

Tegafur-Uracil is an orally active fluoropyrimidines anticancer agent. Tegafur-Uracil inhibits thymidylate synthase. Tegafur-Uracil can be used for researching anti solid tumors[1].

分子量

312.25

Formula

C12H13FN4O5

CAS 号

74578-38-4

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]. Casado E, et al. UFT (tegafur-uracil) in rectal cancer. Ann Oncol. 2008;19(8):1371-1378.

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PI3K-IN-31

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。

PI3K-IN-31 

PI3K-IN-31 (Compound 6b) 是一种有效的 PI3K 抑制剂,对 PI3KαPI3KβPI3KγPI3KδIC50 分别为 3.7 nM、74 nM、14.6 nM 和 9.9 nM。PI3K-IN-31 具有抗癌作用。

PI3K-IN-31

PI3K-IN-31 Chemical Structure

CAS No. : 1359956-12-9

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生物活性

PI3K-IN-31 (Compound 6b) is a potent PI3K inhibitor with IC50s of 3.7 nM, 74 nM, 14.6 nM, and 9.9 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively. PI3K-IN-31 has anticancer effects[1].

IC50 & Target[1]

PI3Kα

3.7 nM (IC50)

PI3Kδ

9.9 nM (IC50)

PI3Kγ

14.6 nM (IC50)

PI3Kβ

74 nM (IC50)

分子量

435.43

Formula

C19H23F2N7O3

CAS 号

1359956-12-9

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]. Marcian E Van Dort, et al. Structural effects of morpholine replacement in ZSTK474 on Class I PI3K isoform inhibition: Development of novel MEK/PI3K bifunctional inhibitors. Eur J Med Chem. 2022 Feb 5;229:113996.

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KRAS G12D inhibitor 10

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。

KRAS G12D inhibitor 10 

KRAS G12D inhibitor 10 是一种有效的 KRAS G12D 抑制剂。Ras 蛋白家族是一种重要的细胞内信号分子,在生长发育中起重要作用。KRAS G12D inhibitor 10 具有研究 KRAS G12D 介导的癌症的潜力 (摘自专利 WO2021108683A1,化合物 34)。

KRAS G12D inhibitor 10

KRAS G12D inhibitor 10 Chemical Structure

CAS No. : 2648551-54-4

规格 是否有货
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250 mg   询价  
500 mg   询价  

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生物活性

KRAS G12D inhibitor 10 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 10 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 34)[1].

分子量

617.18

Formula

C33H41ClN8O2

CAS 号

2648551-54-4

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]. Jennifer PITZEN, et al. Covalent ras inhibitors and uses thereof. Patent WO2021108683A1.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

KRAS G12D inhibitor 9

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。

KRAS G12D inhibitor 9 

KRAS G12D inhibitor 9 是一种有效的 KRAS G12D 抑制剂。Ras 蛋白家族是一种重要的细胞内信号分子,在生长发育中起重要作用。KRAS G12D inhibitor 9 具有研究 KRAS G12D 介导的癌症的潜力 (摘自专利 WO2021108683A1,化合物 20)。

KRAS G12D inhibitor 9

KRAS G12D inhibitor 9 Chemical Structure

CAS No. : 2648551-39-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

KRAS G12D inhibitor 9 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 9 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 20)[1].

分子量

569.74

Formula

C33H43N7O2

CAS 号

2648551-39-5

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]. Jennifer PITZEN, et al. Covalent ras inhibitors and uses thereof. Patent WO2021108683A1.

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Sulfo-GMBS

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。

Sulfo-GMBS 

Sulfo-GMBS 是一种交联剂。在胺-巯基交联剂中,Sulfo-GMBS 产生的交联数量最多,并覆盖了用 AMAS 和 GMBS 鉴定的大部分交联。

Sulfo-GMBS

Sulfo-GMBS Chemical Structure

CAS No. : 185332-92-7

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生物活性

Sulfo-GMBS is a cross-linker. Among the amine-sulfhydryl cross-linkers, Sulfo-GMBS generated the largest number of cross-links and covered most of the cross-links that were identified with AMAS and GMBS[1].

分子量

382.28

Formula

C12H11N2NaO9S

CAS 号

185332-92-7

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]. Ding YH, et al. Increasing the Depth of Mass-Spectrometry-Based Structural Analysis of Protein Complexes through the Use of Multiple Cross-Linkers. Anal Chem. 2016 Apr 19;88(8):4461-9.

    [2]. Yue-He Ding, et al. Increasing the Depth of Mass-Spectrometry-Based Structural Analysis of Protein Complexes through the Use of Multiple Cross-Linkers. Anal Chem. 2016 Apr 19;88(8):4461-9.

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KRAS G12D inhibitor 13

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。

KRAS G12D inhibitor 13 

KRAS G12D inhibitor 13 是一种有效的 KRAS G12D 抑制剂。Ras 蛋白家族是一种重要的细胞内信号分子,在生长发育中起重要作用。KRAS G12D inhibitor 13 具有研究 KRAS G12D 介导的癌症的潜力 (摘自专利 WO2021108683A1,化合物 142)。

KRAS G12D inhibitor 13

KRAS G12D inhibitor 13 Chemical Structure

CAS No. : 2648552-62-7

规格 是否有货
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生物活性

KRAS G12D inhibitor 13 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 13 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 142)[1].

分子量

589.64

Formula

C31H33F2N7O3

CAS 号

2648552-62-7

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]. Jennifer PITZEN, et al. Covalent ras inhibitors and uses thereof. Patent WO2021108683A1.

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Bizine

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。

Bizine 

Bizine 是一种 Phenelzine 类似物,是有效和选择性的 LSD1 抑制剂,Ki 值为 59 nM。Bizine 可以调节癌细胞中的组蛋白甲基化。Bizine 显示出神经保护作用。

Bizine

Bizine Chemical Structure

CAS No. : 1591932-50-1

规格 是否有货
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生物活性

Bizine, a Phenelzine analogue, is a potent and selective LSD1 inhibitor, with a b>Ki of 59 nM. Bizine can modulate bulk histone methylation in cancer cells. Bizine shows neuroprotective effects[1].

IC50 & Target

Ki: 59 nM (LSD1)[1]

分子量

297.39

Formula

C18H23N3O

CAS 号

1591932-50-1

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]. Prusevich P, et, al. A selective phenelzine analogue inhibitor of histone demethylase LSD1. ACS Chem Biol. 2014 Jun 20;9(6):1284-93.

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KRAS G12D inhibitor 10

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。

KRAS G12D inhibitor 10 

KRAS G12D inhibitor 10 是一种有效的 KRAS G12D 抑制剂。Ras 蛋白家族是一种重要的细胞内信号分子,在生长发育中起重要作用。KRAS G12D inhibitor 10 具有研究 KRAS G12D 介导的癌症的潜力 (摘自专利 WO2021108683A1,化合物 34)。

KRAS G12D inhibitor 10

KRAS G12D inhibitor 10 Chemical Structure

CAS No. : 2648551-54-4

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

KRAS G12D inhibitor 10 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 10 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 34)[1].

分子量

617.18

Formula

C33H41ClN8O2

CAS 号

2648551-54-4

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]. Jennifer PITZEN, et al. Covalent ras inhibitors and uses thereof. Patent WO2021108683A1.

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TNIK-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。

TNIK-IN-4 

TNIK-IN-4 是一种有效的 TNIK 抑制剂,IC50 为 0.61 μM。TNIK-IN-4 对典型的结直肠癌细胞系 HCT116 具有抑制活性。

TNIK-IN-4

TNIK-IN-4 Chemical Structure

CAS No. : 2754266-04-9

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生物活性

TNIK-IN-4 is a potent TNIK inhibitor with IC50 of 0.61 μM. TNIK-IN-4 has inhibitory activity against typical colorectal cancer cell line HCT116[1].

IC50 & Target

IC50: 0.61 μM (TNIK)[1]

体外研究
(In Vitro)

TNIK-IN-4 (compound 5a) (0.4-100 μM; 72 hours) has inhibitory activity against typical colorectal cancer cell line HCT116 with IC50 of 36.423 μM[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: HCT116 cells[1]
Concentration: 0.4, 1.2, 3.7, 11.1, 33.3 and 100 μM
Incubation Time: 72 hours
Result: Showed inhibitory activity against typical colorectal cancer cell line HCT116 with IC50 of 36.423 μM.

分子量

365.36

Formula

C20H16FN3O3

CAS 号

2754266-04-9

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]. Luo X, Yang R, Li Y, Zhang L, Yang S, Li L. Discovery of benzo[d]oxazol-2(3H)-one derivatives as a new class of TNIK inhibitors for the treatment of colorectal cancer. Bioorg Med Chem Lett. 2022;67:128745.

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(E/Z)-ZL0420

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。

(E/Z)-ZL0420 

(E/Z)-ZL0420 是 (Z)-ZL0420 和 (E)-ZL0420 的消旋体。(E)-ZL0420 是有效且选择性的 BET 溴结构域 4 (BRD4) 抑制剂,对 BRD4 BD1 和 BRD4 BD2 的 IC50 分别为 27 nM 和 32 nM。

(E/Z)-ZL0420

(E/Z)-ZL0420 Chemical Structure

CAS No. : 2229039-45-4

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生物活性

(E/Z)-ZL0420 is a racemic compound of (Z)-ZL0420 and (E)-ZL0420 isomers. (E)-ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2[1].

分子量

296.32

Formula

C16H16N4O2

CAS 号

2229039-45-4

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]. Zhiqing Liu, et al. Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. Eur J Med Chem. 2018 May 10;151:450-461.

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KRAS G12D inhibitor 13

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。

KRAS G12D inhibitor 13 

KRAS G12D inhibitor 13 是一种有效的 KRAS G12D 抑制剂。Ras 蛋白家族是一种重要的细胞内信号分子,在生长发育中起重要作用。KRAS G12D inhibitor 13 具有研究 KRAS G12D 介导的癌症的潜力 (摘自专利 WO2021108683A1,化合物 142)。

KRAS G12D inhibitor 13

KRAS G12D inhibitor 13 Chemical Structure

CAS No. : 2648552-62-7

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生物活性

KRAS G12D inhibitor 13 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 13 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 142)[1].

分子量

589.64

Formula

C31H33F2N7O3

CAS 号

2648552-62-7

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]. Jennifer PITZEN, et al. Covalent ras inhibitors and uses thereof. Patent WO2021108683A1.

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EGFR-IN-48

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。

EGFR-IN-48 

EGFR-IN-48 是一种有效的且具有口服活性的 EGFR 抑制剂,对 EGFRd19/TM/CS, EGFRLR/TM/CS, EGFRWTIC50 值分别为 0.193 nM, 0.251 nM, 10.4 nM。EGFR-IN-48 抑制 BaF3EGFR del19/T790M/C797S 和 PC-9EGFR del19/T790M/C797S 细胞的增殖,IC50 值分别为 1.526 nM 和 66.7 nM。

EGFR-IN-48

EGFR-IN-48 Chemical Structure

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生物活性

EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC50s of 0.193 nM, 0.251 nM, 10.4 nM for EGFRd19/TM/CS, EGFRLR/TM/CS, EGFRWT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively[1].

IC50 & Target

EGFRd19/TM/CS

0.193 nM (IC50)

EGFRLR/TM/CS

0.251 nM (IC50)

EGFRWT

10.4 nM (IC50)

体外研究
(In Vitro)

EGFR-IN-48 (compound 23) (10 nM) shows anti-proliferative activities against BaF3EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively[1].
EGFR-IN-48 exhibits potent inhibitory activities against various clinically relevant EGFR mutants with IC50s of 10.4, 3.1, 0.9, 0.1, 0.2, 0.3, 0.2 nM for EGFRWT, EGFRLR, EGFRdel19, EGFRdel19/TM, EGFRLR/TM, EGFRLR/TM/CS, EGFRdrl19/TM/CS, respectively[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: BaF3EGFR del19/T790M/C797S, PC-9EGFR del19/T790M/C797S cells
Concentration: 10 nM
Incubation Time:
Result: Showed anti-proliferative activities against BaF3EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively.

体内研究
(In Vivo)

EGFR-IN-48 (2 mg/kg for i.v.; 10 mg/kg for o.p.) shows good oral bioavailability and high plasma exposure in CD-1 mouse[1]. Pharmacokinetic Parameters of EGFR-IN-48 in CD-1 mouse[1].

Route Dose (mg/kg) Vdss (L/kg) T1/2 (h) CL (L/h/kg) AUC0-last (h*ng/mL) Cmax (ng/mL) Tmax (h) F (%)
i.v. 2 0.7 3.3 2.4 13820.0
p.o. 10 33811.0 6600.0 0.5 48.9

CD-1 mouse; 2 mg/kg for i.v.; 10 mg/kg for o.p.[1].

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

Animal Model: CD-1 mouse[1]
Dosage:
Administration: 2 mg/kg for i.v.; 10 mg/kg for o.p.
Result: Showed good oral bioavailability and high plasma exposure.

分子量

800.75

Formula

C35H47BrN9O4PS

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]. Fang H, et al. Design, synthesis and evaluation of the Brigatinib analogues as potent inhibitors against tertiary EGFR mutants (EGFRdel19/T790M/C797S and EGFRL858R/T790M/C797S). Bioorg Med Chem Lett. 2022; 9:128729.

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Hydroxytanshinone IIA

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。

Hydroxytanshinone IIA 

Hydroxytanshinone IIA 是 Tanshinone IIA 的水解代谢物。Tanshinone IIA 可以通过靶向 VEGF/VEGFR2 的蛋白激酶结构域来抑制血管生成。

Hydroxytanshinone IIA

Hydroxytanshinone IIA Chemical Structure

CAS No. : 18887-18-8

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生物活性

Hydroxytanshinone IIA is a hydroxylated metabolite of Tanshinone IIA. Tanshinone IIA may suppress angiogenesis by targeting the protein kinase domains of VEGF/VEGFR2[1].

分子量

310.34

Formula

C19H18O4

CAS 号

18887-18-8

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]. Peng Li, et al. Simultaneous determination of tanshinone IIA and its three hydroxylated metabolites by liquid chromatography/tandem mass spectrometry. Rapid Commun Mass Spectrom. 2006;20(5):815-22.

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TNIK-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。

TNIK-IN-4 

TNIK-IN-4 是一种有效的 TNIK 抑制剂,IC50 为 0.61 μM。TNIK-IN-4 对典型的结直肠癌细胞系 HCT116 具有抑制活性。

TNIK-IN-4

TNIK-IN-4 Chemical Structure

CAS No. : 2754266-04-9

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

TNIK-IN-4 is a potent TNIK inhibitor with IC50 of 0.61 μM. TNIK-IN-4 has inhibitory activity against typical colorectal cancer cell line HCT116[1].

IC50 & Target

IC50: 0.61 μM (TNIK)[1]

体外研究
(In Vitro)

TNIK-IN-4 (compound 5a) (0.4-100 μM; 72 hours) has inhibitory activity against typical colorectal cancer cell line HCT116 with IC50 of 36.423 μM[1].

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.

Cell Proliferation Assay

Cell Line: HCT116 cells[1]
Concentration: 0.4, 1.2, 3.7, 11.1, 33.3 and 100 μM
Incubation Time: 72 hours
Result: Showed inhibitory activity against typical colorectal cancer cell line HCT116 with IC50 of 36.423 μM.

分子量

365.36

Formula

C20H16FN3O3

CAS 号

2754266-04-9

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]. Luo X, Yang R, Li Y, Zhang L, Yang S, Li L. Discovery of benzo[d]oxazol-2(3H)-one derivatives as a new class of TNIK inhibitors for the treatment of colorectal cancer. Bioorg Med Chem Lett. 2022;67:128745.

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Sulfo-GMBS

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。

Sulfo-GMBS 

Sulfo-GMBS 是一种交联剂。在胺-巯基交联剂中,Sulfo-GMBS 产生的交联数量最多,并覆盖了用 AMAS 和 GMBS 鉴定的大部分交联。

Sulfo-GMBS

Sulfo-GMBS Chemical Structure

CAS No. : 185332-92-7

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生物活性

Sulfo-GMBS is a cross-linker. Among the amine-sulfhydryl cross-linkers, Sulfo-GMBS generated the largest number of cross-links and covered most of the cross-links that were identified with AMAS and GMBS[1].

分子量

382.28

Formula

C12H11N2NaO9S

CAS 号

185332-92-7

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]. Ding YH, et al. Increasing the Depth of Mass-Spectrometry-Based Structural Analysis of Protein Complexes through the Use of Multiple Cross-Linkers. Anal Chem. 2016 Apr 19;88(8):4461-9.

    [2]. Yue-He Ding, et al. Increasing the Depth of Mass-Spectrometry-Based Structural Analysis of Protein Complexes through the Use of Multiple Cross-Linkers. Anal Chem. 2016 Apr 19;88(8):4461-9.

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Desmethyl-VS-5584(Synonyms: Desmethyl-SB2343)

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。

Desmethyl-VS-5584 (Synonyms: Desmethyl-SB2343)

Desmethyl-VS-5584 是 VS-5584 的二甲基类似物,VS-5584 是一种具有吡啶 [2,3-d] 嘧啶结构的有效且有选择性 mTOR/PI3K 双重抑制剂。

Desmethyl-VS-5584(Synonyms: Desmethyl-SB2343)

Desmethyl-VS-5584 Chemical Structure

CAS No. : 1246535-95-4

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生物活性

Desmethyl-VS-5584 is a dimethyl analog of VS-5584 which is an potent and selective mTOR/PI3K dual inhibitor with pyrido [2,3-d] pyrimidine structure[1].

分子量

340.38

Formula

C16H20N8O

CAS 号

1246535-95-4

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]. Hart S, Novotny-Diermayr V, Goh KC, et al. VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer. Mol Cancer Ther. 2013;12(2):151-161.

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