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16

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9304	(S)-Sunvozertinib N-[5-[[4-[5-Chloro-4-fluoro-2-(2-hydroxypropan-2-yl)anilino]pyrimidin-2-yl]amino]-2-[(3S)-3-(dimethylamino)pyrrolidin-1-yl]-4-methoxyphenyl]prop-2-enamide,DZD9008	EGFR; HER	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	(S)-Sunvozertinib (DZD9008) 是 Sunvozertinib 的 S-对映体，能够抑制EGFR 外显子 20 NPH 和 ASV 插入、EGFR L858R/T790M 突变及 Her2 外显子 20 YVMA 插入，也能够抑制BTK。
T1797	Cabozantinib S-malate 苹果酸卡博替尼,Cabozantinib,卡博替尼苹果酸盐,XL184,Cabozantinib Malate	Apoptosis; VEGFR; c-Met/HGFR; TAM Receptor; c-Kit	Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors
	Cabozantinib S-malate (XL184) 是一种多受体酪氨酸激酶抑制剂，抑制VEGFR2，c-Met，Kit，Axl 和Flt3的IC50分别为0.035，1.3，4.6，7 和 11.3 nM。
T11213	Epertinib hydrochloride S-22611 hydrochloride	EGFR; HER	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Epertinib hydrochloride (S-22611 hydrochloride) 是口服可逆的选择性EGFR、HER2和HER4抑制剂，IC50值分别为 1.48、7.15 和 2.49 nM，具有抗肿瘤活性。
T4075	Sulfatinib KDR-IN-1,索凡替尼	VEGFR; FGFR; HER	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Sulfatinib (KDR-IN-1) (HMPL-012) 是一种有效且高度选择性的酪氨酸激酶抑制剂，可抑制VEGFR1/2/3，FGFR1和CSF1R，IC50范围为1 到 24 nM 之间。
T11378	GDC-0834 S-enantiomer	Others	Others
	GDC-0834, the S-enantiomer, is a potent and selective inhibitor of Bruton's tyrosine kinase (BTK).
T39906	LAS17 LAS17
	LAS17 is a potent and selective tyrosine-directed irreversible inhibitor for glutathione S-Transferase Pi ( GSTP1 ). LAS17 inhibits GSTP1 activity with an IC 50 of 0.5 μM.
T36429	Dihydrodiol-Ibrutinib
	PCI 45227 is an active metabolite of the Bruton's tyrosine kinase inhibitor ibrutinib .1PCI 45227 is formed from ibrutinib by the cytochrome P450 (CYP) isoform CYP3A. 1.Veeraraghavan, S., Viswanadha, S., Thappali, S., et al.Simultaneous quantification of lenalidomide, ibrutinib and its active metabolite PCI-45227 in rat plasma by LC-MS/MS: Application to a pharmacokinetic studyJ. Pharm. Biomed. Anal.107151-158(2015)
T68523	AMG-628, (S)-
	AMG-628, (S)-, is the S isomer of AMG-628 --- a potent, ATP-competitive inhibitor of Raf kinases. AMG-628 displays selectivity for Raf kinases and inhibits activation of tyrosine protein kinases such as VEGFR2, Lyn, Flt1 and Fms. AMG-628 has shown to inhibit growth, and induces cell cycle arrest and apoptosis in colon and melanoma cell lines with the B-RafV600E mutation.
T37393	13(S)-HpODE
	13(S)-HpODE is produced by the oxidation of linoleic acid by lipoxygenase-1 (LO-1) in many plants including soybean, flaxseed, apples, and tea leaves,1,2 and by 15-LO in mammals.3 In plants, 13(S)-HpODE is the preferred substrate for the garlic bulb divinyl ether synthase.4 In mammalian tissues, 13(S)-HpODE is generally reduced to 13(S)-HODE，a compound which exhibits many biological activities.3 A direct action for 13(S)-HpODE has been demonstrated in Syrian hamster embryo cells where it stimula...
T37079	VEGFR2 Kinase Inhibitor II
	Vascular endothelial growth factor receptor 2 (VEGFR2, also known as KDR and FLK1) is a receptor tyrosine kinase that regulates angiogenesis, vascular development, and embryonic hematopoiesis in response to VEGF isoforms A, C, and D. VEGFR2 kinase inhibitor II is a reversible, cell-permeable inhibitor of VEGFR2's kinase activity (IC50 = 70 nM). It less potently inhibits the platelet-derived growth factor receptor β (PDGFRβ; IC50 = 920 nM) and related receptor and non-receptor tyrosine kinases. V...
T36367	RK-682 (calcium salt)
	Protein tyrosine phosphatases (PTPs) remove phosphate from tyrosine residues of cellular proteins. Reversible phosphorylation catalyzed by the coordinated actions of protein tyrosine kinases and phosphatases is key to the regulation of the signaling events that control cell growth and proliferation, differentiation, and survival or apoptosis, as well as adhesion and motility. RK-682, a bioactive compound originally isolated from the fermentation of Streptomyces sp. 88-682, is an inhibitor of the...
T71811	Lobaric acid
	Lobaric acid is a depsidone metabolite that has been isolated from Stereocaulon lichen species with antioxidant, antiproliferative, antiviral, and enzyme inhibitory activites. It scavenges superoxide radicals in a cell-free assay (IC50 = 97.9 μmol) and inhibits proliferation in a panel of leukemia, colorectal, gastric, breast, ovarian, prostate, pancreatic, and lung cancer cell lines (EC50s = 15.2-63.9 μg/ml). Lobaric acid inhibits protein tyrosine phosphatase 1B (PTP1B; IC50 = 0.87 μM for the h...
T68581	AP23464
	AP23464 is a potent adenosine 5'-triphosphate (ATP)-based inhibitor of Src and Abl kinases, displays antiproliferative activity against a human CML cell line and Bcr-Abl-transduced Ba/F3 cells (IC(50) = 14 nM. AP23464 ablates Bcr-Abl tyrosine phosphorylation, blocks cell cycle progression, and promotes apoptosis of Bcr-Abl-expressing cells. Biochemical assays with purified glutathione S transferase (GST)-Abl kinase domain confirmed that AP23464 directly inhibits Abl activity. Importantly, the lo...
T82971	ARI-1
	ARI-1是一种针对受体酪氨酸激酶样孤儿受体ROR1的抑制剂，对于ROR1异常表达所致的非小细胞肺癌(NSCLC)及EGFR-TKI诱导的耐药性治疗具有显著效果。该化合物能够特异性结合至ROR1的胞外卷曲结构域，并以ROR1依赖性方式抑制PI3K/AKT/mTOR信号通路，进而有效地阻断NSCLC细胞的增殖和迁移。此外，ARI-1还展现了显著的体内抗肿瘤活性。
T36055	Nitisinone-13C6 Nitisinone-13C6
	Nitisinone-13C6is intended for use as an internal standard for the quantification of nitisinone by GC- or LC-MS. Nitisinone is an inhibitor of 4-hydroxyphenylpyruvate dioxygenase (HPPD), which converts 4-hydroxyphenylpyruvate (HPPA) to homogentisate in the tyrosine catabolic pathway.1Nitisinone increases urinary levels of HPPA and 4-hydroxyphenyllactate (HPLA) in rats when administered at a dose of 10 mg/kg. Nitisinone (3 mg/kg) prevents the neonatal lethality of fumarylacetoacetate hydrolase (F...
T36648	Tucatinib hemiethanolate
	Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM. Tucatinib hemiethanolate has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 versus EGFR in cell-based assays. Tucatinib selectively inhibits the receptor tyrosine kinase HER2 relative to EGFR[1].Tucatinib blocks proliferation and the phosphorylation of HER2 and its downstream effector, Akt in HER2 overexpressing cell lines. In the ...

化合物

(S)-Sunvozertinib

Cat.No: T9304

Synonym: N-[5-[[4-[5-Chloro-4-fluoro-2-(2-hydroxypropan-2-yl)anilino]pyrimidin-2-yl]amino]-2-[(3S)-3-(dimethylamino)pyrrolidin-1-yl]-4-methoxyphenyl]prop-2-enamide,DZD9008

Target: EGFR, HER

Cabozantinib S-malate

Cat.No: T1797

Synonym: 苹果酸卡博替尼,Cabozantinib,卡博替尼苹果酸盐,XL184,Cabozantinib Malate

Target: Apoptosis, VEGFR, c-Met/HGFR, TAM Receptor, c-Kit

Epertinib hydrochloride

Cat.No: T11213

Synonym: S-22611 hydrochloride

Target: EGFR, HER

Cat.No: T4075

Synonym: KDR-IN-1,索凡替尼

Target: VEGFR, FGFR, HER

GDC-0834 S-enantiomer

Cat.No: T11378

Target: Others

Cat.No: T39906

Synonym: LAS17

Dihydrodiol-Ibrutinib

Cat.No: T36429

Cat.No: T68523

Cat.No: T37393

VEGFR2 Kinase Inhibitor II

Cat.No: T37079

RK-682 (calcium salt)

Cat.No: T36367

Cat.No: T71811

Cat.No: T68581

Cat.No: T82971

Nitisinone-13C6

Cat.No: T36055

Synonym: Nitisinone-13C6

Tucatinib hemiethanolate

Cat.No: T36648

Cat. No.	Product Name	Target	Signaling Pathways
T0493	L-Tyrosine Tyrosine,P-Tyrosine,L-酪氨酸,L-p-Tyrosine,(S)-Tyrosine,酪氨酸	Amino Acids and Derivatives; Endogenous Metabolite	Metabolism
	L-Tyrosine ((S)-Tyrosine) 是一种非必需氨基酸，对后部皮层中柠檬酸合成酶具有抑制活性。
T5290	(S)-2-Hydroxy-3-phenylpropanoic acid L-(−)-3-Phenyllactic acid,L-3-苯乳酸	Others; Endogenous Metabolite	Metabolism; Others
	(S)-2-Hydroxy-3-phenylpropanoic acid (L-(−)-3-Phenyllactic acid) 是苯丙氨酸的代谢产物。苯丙酮尿症患者体液中苯丙氨酸的水平升高。
T75563	Vanicoside E
	Vanicoside E 是一种抗氧化和抗癌剂。Vanicoside E 抑制L-Tyrosine 和L-DOPA，IC50为 45.23 μM 和 189.96 μM。
T38587	Chrysophanol triglucoside
	Chrysophanol triglucoside is an anthraquinone isolated from Cassia obtusifolia , inhibits protein tyrosine phosphatases 1B (PTP1B) and α-glucosidase with IC 50 s of 80.17 and 197.06 μM, respectively. Chrysophanol triglucoside has the potential for diabetes research.

天然产物

Cat.No: T0493

Synonym: Tyrosine,P-Tyrosine,L-酪氨酸,L-p-Tyrosine,(S)-Tyrosine,酪氨酸

Target: Amino Acids and Derivatives, Endogenous Metabolite

(S)-2-Hydroxy-3-phenylpropanoic acid

Cat.No: T5290

Synonym: L-(−)-3-Phenyllactic acid,L-3-苯乳酸

Target: Others, Endogenous Metabolite

Cat.No: T75563

Chrysophanol triglucoside

Cat.No: T38587

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