首页工具

登录

搜索结果

Search Results for " mutated "

63

抑制剂 & 化合物

2

天然产物

如果没找到您满意的产品或者您对产品有其他要求，可以联系我们专业顾问为您提供针对性的合理建议。 QQ咨询网站留言咨询

Cat. No.	Product Name	Target	Signaling Pathways
T16162	Mutated EGFR-IN-1 Osimertinib analog,AZD9291中间体1	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Mutated EGFR-IN-1 (Osimertinib analog) 是用于突变 EGFR 抑制剂设计的有用中间体，例如 L858R EGFR、Exon19 缺失激活突变体和 T790M 抗性突变体。
T12130	Mutated EGFR-IN-2	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Mutated EGFR-IN-2 is an inhibitor of mutant-selective EGFR.
T12131	Mutated EGFR-IN-3	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Mutated EGFR-IN-3 is a ATP-competitive and highly selective allosteric dibenzodiazepinone EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) inhibitor(IC50 of 12 nM and 13 nM, respectively. )
T5175	azd1390	ATM/ATR	DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	AZD1390 是一种可口服的，可渗透脑的ATM 高度选择性抑制剂，IC50为 0.78 nM。
T1958	AZ20	ATM/ATR; mTOR	DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	AZ20 是一种有效且特异性的 ATR 激酶抑制剂，IC50值为 5 nM。它还抑制mTOR 活性，IC50值为 38 nM。
T4443	AZ32	ATM/ATR	DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	AZ32 是一种口服生物利用度和血脑屏障穿透性 ATM 抑制剂，对 ATM 酶的 IC50 <6.2 nM，对细胞内 ATM 的 IC50 为 0.31 μM。
T6770	AZD0156	Apoptosis; ATM/ATR	Apoptosis; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	AZD0156 是一种口服活性 ATM 选择性抑制剂，IC50为 0.58 nM。它抑制 ATM 介导的信号转导，防止 DNA 损伤检查点激活，破坏 DNA 损伤修复，起抗肿瘤作用。
T6261	CP-466722 CP 466722,CP466722	ATM/ATR	DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	CP-466722 是一种有效且可逆的 ATM 抑制剂，IC50值为 4.1 μM。它不会抑制细胞中的 ATR 和 PI3K 或 PIKK 家族成员。
T1821	CGK733 CGK 733	ATM/ATR	DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	CGK733 (CGK 733) 是一种有效的选择性 ATM/ATR 抑制剂，用于癌症研究。
T6734	WZ8040	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	WZ8040 是一种新型突变选择性不可逆 EGFRT790M 抑制剂，可抑制EGFR 磷酸化。它对突变型EGFR 的活性是野生型EGFR 的100倍以上。
T3338	Ceralasertib AZD6738	ATM/ATR	DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	Ceralasertib (AZD6738) 是一种具有口服活性的选择性 ATR 激酶抑制剂，IC50 为 1 nM。
T2084	ETP-46464	ATM/ATR; DNA-PK; PI3K; mTOR	DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	ETP-46464 是一种有效且特异性的 ATR 抑制剂，IC50为 25 nM。
T3032	VE-821 ATR Inhibitor IV	ATM/ATR	DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	VE-821 (ATR Inhibitor IV) 是一种有效的 ATP 竞争性的ATR 抑制剂，Ki 为 13 nM，IC50为 26 nM。
T6612	NU6027	ATM/ATR; DNA-PK; CDK	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	NU6027 是一种有效的 ATR/CDK 抑制剂，抑制 CDK1/2、ATR 和 DNA-PK，Ki 为 2.5 μM/1.3 μM、0.4 μM 和 2.2 μM。它以 ATR 依赖性方式增强羟基脲和顺铂的细胞毒性。
T7122	AZD-7648	DNA-PK	DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	AZD-7648 是一种 DNA 依赖性蛋白激酶 (DNA-PK) 抑制剂，在酶试验中 IC50 为 0.63 nM，具有抗肿瘤活性。
T2685	KU-55933 ATM Kinase Inhibitor	ATM/ATR; DNA-PK; PI3K; mTOR; Autophagy	Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	KU-55933 (ATM Kinase Inhibitor) 是一种 ATM 抑制剂，IC50和 Ki 值分别为 12.9 和 2.2 nM。它对 ATM 的选择性比对 PI3K/PI4K、 DNA-PK、ATR 和 mTOR 高。
T7318	Elimusertib BAY-1895344	ATM/ATR	DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	Elimusertib (BAY-1895344) 是一种可口服的选择性ATR 抑制剂，IC50值为 7 nM。它具有抗肿瘤活性，可研究实体瘤和淋巴瘤。
T14511	BAY1082439 N-[8-[[(2R)-2-羟基-3-(吗啉-4-基)丙基]氧基]-7-甲氧基-2,3-二氢咪唑并[1,2-C]喹唑啉-5-基]-2-甲基吡啶-3-甲酰胺	Apoptosis; PI3K	Apoptosis; PI3K/Akt/mTOR signaling
	BAY1082439 是一种具有口服活性的，选择性 PI3Kα/β/δ抑制剂。它也能抑制 PIK3CA 的突变形式，它对抑制 Pten 丢失的前列腺癌的生长有很强的作用。
T6487	Encorafenib LGX818	Raf	MAPK
	Encorafenib (LGX818) 是一种可口服的突变型 BRaf V600E 抑制剂，IC50为 0.3 nM，具有潜在的抗肿瘤活性。
T2705	Mutant EGFR inhibitor	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Mutant EGFR inhibitor 是选择性EGFR 突变体抑制剂，可抑制EGFRL858R、EGFRExon 19 deletion 和EGFRT790M。
T9303	MRTX1133	Ras	GPCR/G Protein; MAPK
	MRTX1133 是一种 KRAS G12D 抑制剂 (KD=0.2 pM)，具有强效性、选择性和非共价性。MRTX1133 对 KRAS G12D 突变的肿瘤具有抑制活性，而对 KRAS 野生型肿瘤无抑制活性。
T3579	PLX8394	Raf	MAPK
	PLX8394 是一种口服活性的丝氨酸/苏氨酸蛋白激酶 B-Raf (BRAF) 蛋白抑制剂。 PLX8394 可以选择性地结合并抑制野生型和突变形式的 BRAF 的活性，然后抑制表达 BRAF 突变形式的肿瘤细胞的增殖。 PLX8394 似乎对表达多种激酶突变形式的肿瘤有效，并且可能是对其他对 BRAF V600E 突变体特异的 BRAF 抑制剂疗法耐药的肿瘤的有效治疗剂。
T72771	p53 Activator 7
	p53 Activator 7 是一种 p53突变 Y220C(MDM-2/p53) 激活剂，EC50为 104 nM。p53 Activator 7 可以结合 p53 突变体并恢复其结合 DNA 的能力。
T8882	Vodobatinib K-0706	Bcr-Abl	Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	Vodobatinib (K-0706) 是第三代具有口服活性的Bcr-Abl1酪氨酸激酶抑制剂，IC50=7 nM，对大多数 BCR-ABL1 点突变体具有活性，但对 BCR-ABL1T315I 无活性。它可用于研究慢性粒细胞白血病 (CML)。
T9856	FLT3-IN-10 2-Oxazolamine, 5-(4-fluorophenyl)-N-phenyl-	FLT	Angiogenesis; Tyrosine Kinase/Adaptors
	FLT3-IN-10 (2-Oxazolamine, 5-(4-fluorophenyl)-N-phenyl-) (compound 7c) 是有效的 FMS 样酪氨酸激酶 3 (FLT3) 抑制剂。FLT3-IN-10 具有治疗 FLT3 突变的急性髓性白血病 (AML) 的潜力。
T9473	4SC-203	FLT	Angiogenesis; Tyrosine Kinase/Adaptors
	4SC-203 是一种具有潜在的抗肿瘤活性的多激酶抑制剂。它对 FLT3/STK1、 FLT3 的突变形式以及 VEGFRs 具有选择性抑制作用。
T3024	Avitinib AC0010,艾维替尼	EGFR; JAK; BTK	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors
	Avitinib (AC0010) 是一种不可逆的、突变体选择性的EGFR 抑制剂，可有效抑制非小细胞肺癌中EGFR T790M 耐药突变。阿比替尼也是一种新型BTK 抑制剂。
T1903	Dabrafenib GSK2118436A,GSK2118436,达拉非尼	Raf	MAPK
	Dabrafenib (GSK2118436A) 是一种 Raf 抑制剂，抑制 C-Raf 和 B-RafV600E (IC50=5/0.6 nM)，具有 ATP 竞争性。Dabrafenib 具有抗肿瘤活性，可用于治疗 B-RafV600E 突变的黑色素瘤。
T13884	Shield-1	Others	Others
	Shield-1 是 FK506 结合蛋白 12 (FKBP) 的特异性、高亲和力和细胞渗透性配体，通过与突变的 FKBP (mtFKBP) 结合来逆转不稳定性，允许 mtFKBP 融合蛋白的条件表达。它可以稳定整个融合蛋白。
T2307	Icotinib Hydrochloride 埃克替尼盐酸盐,盐酸埃克替尼,BPI-2009H	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Icotinib Hydrochloride (BPI-2009H) 是一种口服的基于喹唑啉的表皮生长因子受体 (EGFR) 抑制剂，IC50值为5 nM，具有潜在的抗肿瘤活性。
T2490	Osimertinib AZD-9291,Mereletinib,奥希替尼	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Osimertinib (AZD-9291) 是一种 EGFR 三代抑制剂，抑制二代 EGFR 抑制剂产生的 T790M 耐药突变，具有不可逆性和口服活性。Osimertinib 具有抗肿瘤活性，用于治疗 EGFR 突变的非小细胞肺癌。
T3617	Ivosidenib 艾伏尼布,AG-120	Dehydrogenase; Isocitrate Dehydrogenase (IDH)	Metabolism
	Ivosidenib (AG-120) 是一种口服具有活力的异柠檬酸脱氢酶 1 的突变体酶 (mIDH1 enzyme) 抑制剂，能够使 d-2- hydroxyglutatrate (2-HG) 在体内降低。它具有良好的的安全性和临床活性，具有研究 AML 的潜力。
T70133	BAY-846
	BAY-846 is an allosteric MEK inhibitor with long half-lives, high bioavailabilities, low brain penetration potential and high efficacy in a K-Ras-mutated A549 xenograft model.
T34916	Transtinib
	Transtinib is an effective and irreversible EGFR tyrosine kinase inhibitor (EGFR-TKI) that is active against L858R/T790M mutated NSCLC cell lines and xenografts.
T39523	Antitumor agent-28
	Antitumor agent-28 is a compound that specifically targets and inhibits the activity of the ataxia telangiectasia mutated (ATM) kinase. By doing so, it effectively impedes the progression of ATM-mediated diseases and demonstrates significant anti-cancer activity.
T40212	ATR-IN-4
	ATR-IN-4, a potent inhibitor of ATR (Ataxia telangiectasia mutated gene Rad 3-associated kinase), restricts the growth of DU145 prostate cancer cells and NCI-H460 lung cancer cells, with IC 50 values of 130.9 nM and 41.33 nM, respectively.
T71037	BAY-438
	BAY-438 is an allosteric MEK inhibitor with long half-lives, high bioavailabilities, low brain penetration potential and high efficacy in a K-Ras-mutated A549 xenograft model.
T13627	CP-10	CDK	Cell Cycle/Checkpoint
	CP-10 is a PROTAC with highly selective and remarkable CDK6 degradation (DC50: 2.1 nM). It inhibits the proliferation of several hematopoietic cancer cells including multiple myeloma and can degrade mutated and overexpressed CDK6.
T78711	A011	ATM/ATR	DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	A011，作为一种选择性的ataxia-telangiectasia mutated (ATM)抑制剂，其IC50为1.0 nM，能够在与CPT-11联合应用时，诱导Apoptosis及G2/M期细胞周期阻滞，显示出显著的抗肿瘤活性。
T66481	TG-693
	TG693, an orally available inhibitor of CLK1, promotes the skipping of the endogenous mutated exon 31 in Duchenne muscular dystrophy (DMD) patient-derived cells and increased the production of the functional exon 31-skipped dystrophin protein.
T36245	SJF 1528
	Potent EGFR Degrader (DC50 values are 39.2 nM for wild-type EGFR in OVCAR8 cells and 736 nM for Exon20Ins mutated EGFR in HeLa cells). Also degrades HER2. Comprises the EGFR inhibitor lapatinib (Cat. No. 6811) joined by a linker to a von Hippel-Lindau (VHL) recruiting ligand. Inhibits proliferation of HER2-driven breast cancer cell lines (IC50 = 102 nM for SKBr3 cells).
T37661	LY 2886721 Hydrochloride
	Potent and selective β-secretase (BACE) inhibitor (IC50 values are 10.2 and 20.3 nM for human BACE2 and BACE1, respectively). Displays >5,000-fold selectivity for BACE over other proteases including cathepsin D, pepsin and renin. Inhibits Aβ1-40 and Aβ1-42 production in cells expressing mutated APP. Reduces hippocampal and cortical Aβ and sAPPβ levels in an Alzheimer's disease mouse model.
T68895	CBP-93872
	CBP-93872 is a G2 checkpoint inhibitor. CBP-93872 specifically abrogates the DNA double-stranded break (DSB)-induced G2 checkpoint through inhibiting maintenance. CBP-93872 is an inhibitor of maintenance of the DSB-specific G2 checkpoint and thus might be a strong candidate as the basis for a drug that specifically sensitizes p53-mutated cancer cells to DSB-inducing DNA damage therapy.
T77082	Melredableukin alfa
	Melredableukin alfa (RO-7049665)是一种由人IgG1-κ通过多肽连接子与人突变白细胞介素2(IL2 mutin)融合形成的融合蛋白。它适用于乙型肝炎和溃疡性结肠炎的研究。
T74707	PROTAC FLT3/CDK9 degrader-1
	PROTACFLT3/CDK9 degrader-1 是一种有效的FLT3和CDK9双PROTAC 降解剂。PROTACFLT3/CDK9 degrader-1 诱导细胞凋亡 (Apoptosis) 并有效降解靶蛋白FLT3和 CDK9。PROTACFLT3/CDK9 degrader-1具有研究 FLT3-ITD 突变型 AML 的潜力。
T18680	SD-36	Others	Others
	SD-36, a potent and efficacious PROTAC STAT3 degrader (Kd=~50 nM), exhibits high specificity for STAT3 over other STAT members. It effectively targets both wild-type and mutated STAT3 proteins in cells, inhibiting their transcriptional activity (IC50=10 nM). The compound, consisting of the STAT3 inhibitor SI-109, a linker, and a CRBN ligand Lenalidomide analog for E3 ubiquitin ligase[1], demonstrates significant anti-tumor effects and achieves complete, long-lasting tumor regression in mouse mod...
T83737	LRRKtide TFA Moesin (550-564),Membrane-organizing Extension Spike Protein (550-564)
	LRRKtide是一个针对富含亮氨酸重复激酶2 (LRRK2)的肽基底物，LRRK2是在帕金森病患者中频繁发生突变的酶，对应于膜组织扩展刺突蛋白(moesin)的550-564氨基酸。该化合物用于识别LRRK2的抑制剂。
T39439	Seclidemstat mesylate SP-2577 mesylate
	Seclidemstat mesylate (SP-2577) is a highly effective and reversible inhibitor of KDM1A (LSD1), with a Ki of 31 nM and an IC 50 of 13 nM. It demonstrates significant potential in promoting antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, while also exhibiting inhibitory effects on virus production, viral DNA replication, and late gene expression. Seclidemstat mesylate is a valuable tool for studying Ewing Sarcoma in research settings.
T63386	Pan-RAF kinase inhibitor 1
	Pan-RAF kinase inhibitor 1 是 Pan-RAF 激酶对有效抑制剂，能够抑制 RAF 激酶，调节 MAPK 信号传导，进而影响 RAS 突变肿瘤细胞的增殖。 Pan-RAF kinase inhibitor 1 对研究癌症疾病表现出研究潜力。
T71184	ARQ-736
	ARQ 736 is a potent and selective BRAF inhibitor. ARQ 736 is selectively potent in killing cancer cell lines harboring at least one mutated BRAF allele. BRAF mutations were detected in over 60% of melanomas and may account for a significant proportion of colon cancer patients whose tumors are resistant to anti-EGFR therapy. The B-Raf protein is a key signaling molecule in the mitogen activated protein kinase (MAPK) signaling pathway and has been implicated in the pathogenesis of a variety of ca...

化合物

Mutated EGFR-IN-1

Cat.No: T16162

Synonym: Osimertinib analog,AZD9291中间体1

Target: EGFR

Mutated EGFR-IN-2

Cat.No: T12130

Target: EGFR

Mutated EGFR-IN-3

Cat.No: T12131

Target: EGFR

Cat.No: T5175

Target: ATM/ATR

Cat.No: T1958

Target: ATM/ATR, mTOR

Cat.No: T4443

Target: ATM/ATR

Cat.No: T6770

Target: Apoptosis, ATM/ATR

Cat.No: T6261

Synonym: CP 466722,CP466722

Target: ATM/ATR

Cat.No: T1821

Synonym: CGK 733

Target: ATM/ATR

Cat.No: T6734

Target: EGFR

Cat.No: T3338

Synonym: AZD6738

Target: ATM/ATR

Cat.No: T2084

Target: ATM/ATR, DNA-PK, PI3K, mTOR

Cat.No: T3032

Synonym: ATR Inhibitor IV

Target: ATM/ATR

Cat.No: T6612

Target: ATM/ATR, DNA-PK, CDK

Cat.No: T7122

Target: DNA-PK

Cat.No: T2685

Synonym: ATM Kinase Inhibitor

Target: ATM/ATR, DNA-PK, PI3K, mTOR, Autophagy

Cat.No: T7318

Synonym: BAY-1895344

Target: ATM/ATR

Cat.No: T14511

Synonym: N-[8-[[(2R)-2-羟基-3-(吗啉-4-基)丙基]氧基]-7-甲氧基-2,3-二氢咪唑并[1,2-C]喹唑啉-5-基]-2-甲基吡啶-3-甲酰胺

Target: Apoptosis, PI3K

Cat.No: T6487

Synonym: LGX818

Target: Raf

Mutant EGFR inhibitor

Cat.No: T2705

Target: EGFR

Cat.No: T9303

Target: Ras

Cat.No: T3579

Target: Raf

p53 Activator 7

Cat.No: T72771

Cat.No: T8882

Synonym: K-0706

Target: Bcr-Abl

Cat.No: T9856

Synonym: 2-Oxazolamine, 5-(4-fluorophenyl)-N-phenyl-

Target: FLT

Cat.No: T9473

Target: FLT

Cat.No: T3024

Synonym: AC0010,艾维替尼

Target: EGFR, JAK, BTK

Cat.No: T1903

Synonym: GSK2118436A,GSK2118436,达拉非尼

Target: Raf

Cat.No: T13884

Target: Others

Icotinib Hydrochloride

Cat.No: T2307

Synonym: 埃克替尼盐酸盐,盐酸埃克替尼,BPI-2009H

Target: EGFR

Cat.No: T2490

Synonym: AZD-9291,Mereletinib,奥希替尼

Target: EGFR

Cat.No: T3617

Synonym: 艾伏尼布,AG-120

Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)

Cat.No: T70133

Cat.No: T34916

Antitumor agent-28

Cat.No: T39523

Cat.No: T40212

Cat.No: T71037

Cat.No: T13627

Target: CDK

Cat.No: T78711

Target: ATM/ATR

Cat.No: T66481

Cat.No: T36245

LY 2886721 Hydrochloride

Cat.No: T37661

Cat.No: T68895

Melredableukin alfa

Cat.No: T77082

PROTAC FLT3/CDK9 degrader-1

Cat.No: T74707

Cat.No: T18680

Target: Others

Cat.No: T83737

Synonym: Moesin (550-564),Membrane-organizing Extension Spike Protein (550-564)

Seclidemstat mesylate

Cat.No: T39439

Synonym: SP-2577 mesylate

Pan-RAF kinase inhibitor 1

Cat.No: T63386

Cat.No: T71184

Cat. No.	Product Name	Target	Signaling Pathways
TN1673	Garcinone C 伽升沃 C,伽升沃C	ATM/ATR; CDK; STAT; AChR; Antifection	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; JAK/STAT signaling; Microbiology/Virology; Neuroscience; PI3K/Akt/mTOR signaling; Stem Cells
	Garcinone C 是一种从 Garcinia oblongifolia Champ 中提取的黄酮衍生物，具有抗炎、收敛和促进肉芽的活性。 Garcinone C 是一种 AChE 抑制剂，对某些癌症具有潜在的细胞毒性作用。
T1181	Gefitinib ZD1839,吉非替尼	EGFR; Tyrosine Kinases; Autophagy	Angiogenesis; Autophagy; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Gefitinib (ZD1839) 是一种 EGFR 一代抑制剂，具有口服活性，抑制 EGFR 19 Del 和 L858R 突变。Gefitinib 具有抗肿瘤活性，用于治疗 EGFR 突变的非小细胞肺癌。Gefitinib 用药会产生 EGFR C797S 耐药突变。

天然产物

Cat.No: TN1673

Synonym: 伽升沃 C,伽升沃C

Target: ATM/ATR, CDK, STAT, AChR, Antifection

Cat.No: T1181

Synonym: ZD1839,吉非替尼

Target: EGFR, Tyrosine Kinases, Autophagy

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

Copyright © 2015-2024 TargetMol Chemicals Inc. All rights reserved. 沪ICP备20019793号-4

沪公网安备 31010602006700号

沪公网安备 31010602006700号

TargetMol Loading

联系我们

电话：

400-820-0310

邮箱：

service@tsbiochem.com

QQ：

2881945090（终端用户）

2885109491（经销商）

经销：

终端：

地址：

上海市静安区江场三路238号8楼