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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T8684	Sotorasib AMG-510	Ras	GPCR/G Protein; MAPK
	Sotorasib (AMG-510) 是一种 KRAS G12C 共价抑制剂，具有口服活性和选择性。Sotorasib 与 KRAS G12C 非活性构象的 GDP 状态结合，抑制 KRAS 及其下游信号的传导。Sotorasib 对 KRAS G12C 突变肿瘤具有抑制活性。
T60021	ecMetAP-IN-1	Others	Others
	ecMetAP-IN-1 可用作 QSAR 模型，以使用多元线性回归研究蛋氨酸氨基肽酶抑制剂作为抗癌剂。
T10252L2	ADU-S100 ammonium salt ML RR-S2 CDA ammonium salt,MIW815 ammonium salt	STING	Immunology/Inflammation
	ADU-S100 ammonium salt (ML RR-S2 CDA ammonium salt) 是干扰素基因刺激物的激活剂。 ADU-S100 ammonium salt 可导致有效的全身性肿瘤消退和免疫。
T70388	(S)-Enitociclib VIP152	CDK	Cell Cycle/Checkpoint
	(S)-Enitociclib (VIP152) 是一种选择性 CDK9 抑制剂，通过抑制 RNA 聚合酶 II 介导的转录来诱导 MYC+ 淋巴瘤的完全消退，抑制抗凋亡和促生存蛋白的转录。
T39584	MI-3454
	MI-3454 is a highly potent, orally active, and selective inhibitor of the interaction between menin and MLL1, with an IC50 of 0.51 nM. This compound effectively inhibits the proliferation of leukemic cells and promotes their differentiation, leading to the regression or complete remission of leukemia in mouse models featuring MLL1 rearrangements or NPM1 mutations. This remarkable therapeutic effect is achieved through the downregulation of key genes involved in the development of leukemia.
T15249	Estrogen receptor modulator 1	Estrogen Receptor/ERR	Endocrinology/Hormones
	Estrogen receptor modulator 1 是一种有效的、具有口服活性的、选择性雌激素受体(estrogen receptor)调节剂 (SERM)，其 pIC50为 0.46。它能够诱导 Tamoxifen 耐药、激素非依赖性异种移植瘤的消退。
T36287	Pirtobrutinib	BTK	Angiogenesis; Tyrosine Kinase/Adaptors
	Pirtobrutinib (LOXO-305) is an advanced BTK inhibitor that displays high selectivity and operates through a non-covalent mechanism. This compound effectively inhibits various BTK C481 substitution mutations, leading to tumor regression in BTK-dependent lymphoma tumors in mouse xenograft models. Furthermore, Pirtobrutinib exhibits remarkable selectivity for BTK, with more than a 300-fold difference compared to 370 other kinases tested. Notably, at a concentration of 1 μM, Pirtobrutinib demonstrat...
T6248	XL888	HSP	Cytoskeletal Signaling; Metabolism
	XL888 是一种 ATP 竞争性的 Hsp90 抑制剂，IC50值为 24 nM。
T3678	Entrectinib RXDX-101,恩曲替尼,NMS-E628	Trk receptor; ROS; ALK; Autophagy; ROS Kinase	Angiogenesis; Autophagy; Immunology/Inflammation; Tyrosine Kinase/Adaptors
	Entrectinib (RXDX-101) 是一种可口服的 Trk、ROS1和 ALK 抑制剂，具有抗肿瘤和中枢神经活性，抑制 TrkA、TrkB、TrkC、ROS1 和 ALK 的 IC50值分别为 1、3、5、12 和 7 nM。
T81263	RMC-7977	Ras	GPCR/G Protein; MAPK
	RMC-7977是一种可逆的三重复合RAS抑制剂，对KRAS、NRAS和HRAS的突变型及野生型(WT)变体表现出广谱活性。该化合物能够引发肿瘤消退，在多种依赖RAS的临床前癌症模型中显示出良好的耐受性。此外，RMC-7977还能有效抑制KRASG12C癌瘤模型的生长。[1]
T2576	Brivanib (alaninate) 丙氨酸布立尼布,BMS-582664,Brivanib Alaninate	VEGFR; FGFR; Autophagy	Angiogenesis; Autophagy; Tyrosine Kinase/Adaptors
	Brivanib Alaninate (BMS-582664) 是一种血管内皮生长因子受体 2 (VEGFR2) 抑制剂的丙氨酸盐，IC50值为 25 nM，具有潜在的抗肿瘤活性。它对 VEGFR1 和 FGFR1 适度抑制，对 VEGFR2 的选择性是对 PDGFRβ 的 240 倍。
T39938	M-1211
	M 1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression.
T69479	CGC 11093
	CGC 11093 is a polyamine analog; inhibits growth of human prostate tumor xenografts in nude mice. It may prove useful in promoting regression of choroidal neovascularization.
T22290	CFT-743	Others	Others
	CFT-0743 could inhibits tumor growth (81% regression) potently with PDC50 value of 0.18 nM.
T38050	CP-609754	Transferase	Metabolism
	CP-609754 是高效的、可逆的法尼基转移酶抑制剂，对重组人 H-Ras 和重组 K-Ras 法尼基化的 IC50分别为 0.57 ng/mL 和 46 ng/mL。CP-609754有潜在的抗癌作用。
T11396	GGTI-2418	Transferase	Metabolism
	GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors. GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor.
T35273	YPC-22026 YPC22026,YPC 22026
	YPC-22026 is a novel tumor regression inducer that inhibits the znf143 regulatory gene in the mouse xenotransplantation model.
T40223	EEDi-5273
	EEDi-5273 is a highly potent and orally efficacious inhibitor of EED, with an approximate IC50 value of 0.2 nM. This compound exhibits exceptional activity, capable of achieving complete and persistent regression of tumors.
T41205	3',3'-cGAMP sodium salt
	3',3'-cGAMP sodium salt is a STING agonist. Reduces B cell proliferation and induces apoptosis of malignant B cellsin vitro. Suppresses 5TGM1 multiple myeloma xenograft growth in immunodeficient mice, and induces leukemic regression in Eμ-TCL1 mice.
T63328	AMXI-5001 hydrochloride
	AMXI-5001 hydrochloride 是口服具有活力的、有效的 parp1/2 和微管聚合抑制剂，且IC50 值明显低于现有的临床 PARP1/2 抑制剂。MXI-5001 hydrochloride 对多种人类癌细胞表现出选择性抗肿瘤细胞毒性，能够诱导已建立的肿瘤，包括较大的肿瘤完全消退。
T71023	MI-888 free base
	MI-888 is a potent MDM2 inhibitor (Ki = 0.44 nM) with a superior pharmacokinetic profile and enhanced in vivo efficacy. MI-888 is capable of achieving rapid, complete, and durable tumor regression in two types of xenograft models of human cancer with oral administration and represents the most potent and efficacious MDM2 inhibitor reported to date.
T79461	YK-029A	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	YK-029A为口服活性的EGFR突变抑制剂，特异性针对EGFRT790M及EGFRex20ins。该化合物在PDX模型上对肿瘤展现良好的抑制效果，显示出明显的抗肿瘤活性。
T70356	F-1394
	F-1394 is an acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor. F-1394 both prevents the formation of atherosclerosis and accelerates its regression without affecting the serum TC level, indicating that F-1394 acts directly on the arterial wall. F-1394 significantly reduced neointimal thickening and the extent of macrophages in lesions without affecting serum cholesterol levels. In vitro, F-1394 attenuated foam cell formation in mouse peritoneal macrophages.
T78442	TSPP tetrasodium
	TSPP tetrasodium 作为一种光敏剂, 在癌症与微生物感染治疗中展现出效用（Ex: 413 nm, Em: 640 nm）。
T78211	STX-478	PI3K	PI3K/Akt/mTOR signaling
	STX-478（化合物 80）为口服活性、能穿透血脑屏障、选择性针对突变型构象PI3Kα的抑制剂。STX-478表现出对肿瘤的强效抑制和长期缩减效果，适用于癌症研究。
T32026	GYKI-13324 GYKI 13324,GYKI13324
	GYKI-13324 is bifunctional nitrosoureido derivative and alkylating agent. GYKI-13324 was studied on human colorectal tumor xenograft lines. Given orally in single or multiple daily doses, GYKI-13324 produced long-term or total regression of adenomatous, b
T77115	Plamotamab
	Plamotamab (XmAb-13676) 是一种人源双特异性抗体(bsAb)，目标是CD3和CD20，通过招募细胞毒性T细胞以消灭CD20+表达的肿瘤细胞。在体内，Plamotamab诱导了轻微的血液学反应(MR)并有效促进肿瘤消退。
T70552	Ipatasertib tosylate
	Ipatasertib, also known as GDC0068, is an orally active, potent and selective Akt inhibitor. GDC-0068 blocked Akt signaling both in cultured human cancer cell lines and in tumor xenograft models. Inhibition of Akt activity by GDC-0068 resulted in blockade of cell-cycle progression and reduced viability of cancer cell lines. Markers of Akt activation, including high-basal phospho-Akt levels, PTEN loss, and PIK3CA kinase domain mutations, correlate with sensitivity to GDC-0068. In multiple tumor...
T9684	(Z)-Orantinib
	(Z)-Orantinib ((Z)-SU6668) 是一种有效，选择性，具有口服活性和 ATP 竞争性的 Flk‐1/KDR，PDGFRβ和 FGFR1抑制剂，IC50值分别为 2.1，0.008 和 1.2 μM。(Z)-Orantinib 是有效的抗血管生成和抗肿瘤剂，可诱导已形成的肿瘤消退。
T36201	AZD5582 dihydrochloride AZD 5582 dihydrochloride
	Dimeric Smac mimetic; potent inhibitor of X-linked (XIAP) and cellular (cIAP) inhibitor of apoptosis protein (IC50 values are 15, 15 and 21 nM for XIAP, cIAP1 and cIAP2 respectively). Binds to the BIR3 domain of XIAP to prevent interaction with caspase-9. Causes degradation of cIAP1 and cIAP2 and induces apoptosis in MDA-MB-231 breast cancer cells. Causes tumor regression in MDA-MB-231 xenograft-bearing mice. Hennessy et al (2013) Discovery of a novel class of dimeric Smac mimetics as potent IAP...
T74975	Zn-DPA-maytansinoid conjugate 1
	Zn-DPA-maytansinoid conjugate 1 为一种靶向小分子免疫检查点的类美坦素偶联物。其能持续诱导肿瘤生长消退，并激活肿瘤微环境（TME），转化为“炎热肿瘤”。
T70588	Tazemetostat HCl
	Tazemetostat HCl is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity. EPZ-6438 induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells. Treatment of xenograft-bearing mice with EPZ-6438 leads to dose-dependent regression of MRTs with correlative diminution of intratumoral trimethylation levels of lysine 27 on histone H3, and prevention of tumor regrowth after dosing cessation. These data demonstrate the dependency of SMARCB1...
T64015	FGFR4-IN-6
	FGFR4-IN-6 是一种共价的、可逆的 FGFR4 抑制剂 (IC50: 5.4 nM)，表现出良好的口服药代动力学特性。在 Hep3B2.1-7 HCC 细胞系的异种移植小鼠模型中，FGFR4-IN-6 能够明显诱导肿瘤消退，且无明显的毒性。
T74749	AK-2292
	AK-2292 是一种有效和选择性STAT5PROTAC 降解剂，DC50值为 0.10 μM。AK-2292 在体外和体内诱导 STAT5A/B 蛋白的降解。AK-2292 可在急性髓性白血病和慢性髓性白血病异种移植小鼠模型中诱导肿瘤消退。
T34278	Redaporfin F 2BMet,F2BMet,F-2BMet,LUZ11,LUZ 11,LUZ-11
	Redaporfin, also known as F-2BMet or LUZ-11, is a photosensitizer for Photodynamic Therapy (PDT) of cancer. Redaporfin showed a high efficacy in the treatment of male BALB/c mice with subcutaneously implanted colon (CT26) tumours. Vascular-PDT with 1.5 mg
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...
T78836	IHMT-PI3K-455	PI3K	PI3K/Akt/mTOR signaling
	IHMT-PI3K-455（Compound 15u）为一种高效、选择性且具口服活性的PI3Kγ/δ双重抑制剂，其针对PI3Kγ与PI3Kδ的IC50值分别为7.1 nM和0.57 nM。该化合物能够抑制AKT磷酸化，并通过促进CD8+杀伤性T细胞的招募与激活，抑制肿瘤生长，适用于肿瘤学研究领域。
T9429	ZZW-115
	ZZW-115 是一种有效的 NUPR1抑制剂，Kd 为 2.1 μM。ZZW-115是三氟拉嗪(TFP)的衍生物。ZZW-115显示出剂量依赖性肿瘤消退，无神经系统副作用，主要通过坏死和凋亡诱导细胞死亡。
T62847	AMXI-5001
	AMXI-5001 是一种有效的、口服具有活力的 parp1/2 和微管聚合抑制剂。MXI-5001 对多种人类癌细胞显示出选择性抗肿瘤细胞毒性，其 IC50s 远低于现有的临床 PARP1/2 抑制剂。AMXI-5001 能够诱导已建立的肿瘤（包括很大的肿瘤）完全消退。
T82517	DYSP-C34
	DYSP-C34是一种生物相容性强且有效的超声（US）激活多功能分子机器。它提升了亲脂性/亲水性平衡，增强了超声诱导的ROS产生，并改善了细胞渗透能力，进而显著提升了对肿瘤的靶向效果及声动力疗法（SDT）介导的肿瘤缩减能力。此外，DYSP-C34还通过激活APC展示出温和的免疫原性。
T68497	FI-700
	FI-700 is a novel and potent FLT3 inhibitor with promising antileukemia activity. FI-700 showed a potent IC(50) value against FLT3 kinase at 20 nmol/L in an in vitro kinase assay. FI-700 showed selective growth inhibition against mutant FLT3-expressing leukemia cell lines and primary acute myeloid leukemia cells, whereas it did not affect the FLT3 ligand (FL)-driven growth of Wt-FLT3-expressing cells. Oral administration of FI-700 induced the regression of tumors in a s.c. tumor xenograft model ...
T70779	BPR1J-340
	BPR1J-340 is a potent and selective FLT3 inhibitor with potential anticancer activity. BPR1J-340 was identified as a novel potent FLT3 inhibitor by biochemical kinase activity (IC50 approximately 25 nM) and cellular proliferation (GC50 approximately 5 nM) assays. BPR1J-340 inhibited the phosphorylation of FLT3 and STAT5 and triggered apoptosis in FLT3-ITD(+) AML cells. The pharmacokinetic parameters of BPR1J-340 in rats were determined. BPR1J-340 also demonstrated pronounced tumor growth inhibit...
T78804	PI3Kα-IN-12	PI3K	PI3K/Akt/mTOR signaling
	PI3Kα-IN-12（化合物13），作为一种高度选择性的PI3Kα抑制剂，展现出了1.2 nM的IC50值。在HCT-116和U87-MG细胞线上的抑制作用，IC50s分别为0.83 μM和1.25 μM。通过腹腔注射（IP）给予40 mg/kg的PI3Kα-IN-12，能够有效引起接受U87-MG细胞系异种移植的小鼠模型中的肿瘤退缩。
T68389	LY2457546
	LY2457546 is a potent and orally bioavailable inhibitor of multiple receptor tyrosine kinases involved in angiogenic and tumorigenic signalling. LY2457546 demonstrates potent activity against targets that include VEGFR2 (KDR), PDGFRβ, FLT-3, Tie-2 and members of the Eph family of receptors. In vivo, LY2457546 inhibited VEGF-driven autophosphorylation of lung KDR in the mouse and rat in a dose and concentration dependent manner. LY2457546 was well tolerated and exhibited efficacy in a 13762 synge...
T36314	Wortmannin-Rapamycin Conjugate
	Phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) act synergistically in promoting cancer. Wortmannin is a potent inhibitor of PI3K enzymes, while rapamycin blocks mTOR Complex 1 TORC1. Wortmannin-rapamycin conjugate consists of analogs of 17-hydroxy wortmannin and rapamycin conjugated via a prodrug linker. Hydrolysis of the prodrug linker in vivo releases the inhibitors. The wortmannin-rapamycin conjugate inhibits the growth of HT-29 colon tumors and A498 renal tumors in...
T36404	PRLX-93936
	PRLX-93936 is an analog of erastin that has antitumor activity. It inhibits the hypoxia-inducible factor 1 (HIF-1) signaling pathway under hypoxic conditions (IC50 = 0.09 μM in a cell-based reporter assay). PRLX-93936 (1 μM) also inhibits hypoxia-induced increases in HIF-1α expression in ME-180 cervical cancer cells. It inhibits the growth of HT-1080 fibrosarcoma, OVCAR-5 ovarian cancer, BJELR tumorigenic primary fibroblast, and PANC-1 pancreatic cancer cells with IC50 values of less than 100 nM...
T64277	ODN 1585
	ODN 1585 是一种有效的 IFN 和 TNFα 产生诱导剂，也是一种 NK (natural killer) 的有效刺激剂，可用做疫苗佐剂。ODN 1585 能够增强 CD8+ T 细胞的功能，包括 CD8+ T 细胞介导的 IFN-γ 的产生。ODN 1585 可以诱导小鼠已建立的黑色素瘤消退，对小鼠的疟疾也表现出完全的保护作用。ODN 1585 能够用于研究急性骨髓性白血病 (AML) 和疟疾。
T70222	Ethonafide
	Ethonafide is an anthracene-containing derivative of amonafide that belongs to the azonafide series of anticancer agents. The lack of cross-resistance in multidrug-resistant cancer cell lines and the absence of a quinone and hydroquinone moiety make ethonafide a potentially less cardiotoxic replacement for existing anthracene-containing anticancer agents. Ethonafide was cytotoxic against three human prostate cancer cell lines at nanomolar concentrations. Ethonafide was found to be better tolerat...
T80750	YN14	PROTACs	PROTAC
	YN14是一种高效且选择性的KRASG12C蛋白水解靶向嵌合体(PROTAC)。其能够稳定诱导KRASG12C:YN14:VHL三元复合物，并展现出低结合自由能(ΔG)。YN14对KRASG12C突变型癌细胞的增殖具有抑制作用，显著抑制其生长，并能在MIA PaCa-2异种移植模型中促进肿瘤消退，实现超过100%的肿瘤生长抑制(TGI%)。
T37130	MRTX1133 formic
	MRTX1133 is a highly selective, first-in-class inhibitor of KRAS G12D. MRTX1133 targets the KRAS G12D protein in both active and inactive states. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells[1][2]. MRTX1133 demonstrates dose-dependent inhibition of the KRAS pathway tumor regression in G12D mutant tumor models[2]. [1]. Xiaolun Wang, et al.Kras g12d inhibitors.WO2021041671A1.[2]. KRAS G12D Inhibitor: MRTX1133. [(accessed on 22 April 2021)];2021 Available onli...

化合物

Cat.No: T8684

Synonym: AMG-510

Target: Ras

Cat.No: T60021

Target: Others

ADU-S100 ammonium salt

Cat.No: T10252L2

Synonym: ML RR-S2 CDA ammonium salt,MIW815 ammonium salt

Target: STING

(S)-Enitociclib

Cat.No: T70388

Synonym: VIP152

Target: CDK

Cat.No: T39584

Estrogen receptor modulator 1

Cat.No: T15249

Target: Estrogen Receptor/ERR

Cat.No: T36287

Target: BTK

Cat.No: T6248

Target: HSP

Cat.No: T3678

Synonym: RXDX-101,恩曲替尼,NMS-E628

Target: Trk receptor, ROS, ALK, Autophagy, ROS Kinase

Cat.No: T81263

Target: Ras

Brivanib (alaninate)

Cat.No: T2576

Synonym: 丙氨酸布立尼布,BMS-582664,Brivanib Alaninate

Target: VEGFR, FGFR, Autophagy

Cat.No: T39938

Cat.No: T69479

Cat.No: T22290

Target: Others

Cat.No: T38050

Target: Transferase

Cat.No: T11396

Target: Transferase

Cat.No: T35273

Synonym: YPC22026,YPC 22026

Cat.No: T40223

3',3'-cGAMP sodium salt

Cat.No: T41205

AMXI-5001 hydrochloride

Cat.No: T63328

MI-888 free base

Cat.No: T71023

Cat.No: T79461

Target: EGFR

Cat.No: T70356

TSPP tetrasodium

Cat.No: T78442

Cat.No: T78211

Target: PI3K

Cat.No: T32026

Synonym: GYKI 13324,GYKI13324

Cat.No: T77115

Ipatasertib tosylate

Cat.No: T70552

Cat.No: T9684

AZD5582 dihydrochloride

Cat.No: T36201

Synonym: AZD 5582 dihydrochloride

Zn-DPA-maytansinoid conjugate 1

Cat.No: T74975

Tazemetostat HCl

Cat.No: T70588

Cat.No: T64015

Cat.No: T74749

Cat.No: T34278

Synonym: F 2BMet,F2BMet,F-2BMet,LUZ11,LUZ 11,LUZ-11

Cat.No: T18680

Target: Others

Cat.No: T78836

Target: PI3K

Cat.No: T9429

Cat.No: T62847

Cat.No: T82517

Cat.No: T68497

Cat.No: T70779

Cat.No: T78804

Target: PI3K

Cat.No: T68389

Wortmannin-Rapamycin Conjugate

Cat.No: T36314

Cat.No: T36404

Cat.No: T64277

Cat.No: T70222

Cat.No: T80750

Target: PROTACs

MRTX1133 formic

Cat.No: T37130

Cat. No.	Product Name	Target	Signaling Pathways
T4867	Erucic acid Prifac 2990,芥酸,13(Z)-Docosenoic Acid,cis-13-docosenoic acid	PI3K; Endogenous Metabolite	Metabolism; PI3K/Akt/mTOR signaling
	Erucic acid (13(Z)-Docosenoic Acid) 是单不饱和脂肪酸，分离自萝卜的种子。Erucic acid 可以容易地穿过血脑屏障，使大脑中长链脂肪酸的积累正常化。Erucic acid 能够改善认知障碍并有效预防痴呆。

天然产物

Cat.No: T4867

Synonym: Prifac 2990,芥酸,13(Z)-Docosenoic Acid,cis-13-docosenoic acid

Target: PI3K, Endogenous Metabolite

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