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TAS-116

HSP(HSP90)抑制剂

规格或纯度: 98%

CAS编号: 1260533-36-5
分子式: C₂₅H₂₆N₈O
分子量: 454.53
PubChem编号: 67501411

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货号 (SKU)	包装规格	是否现货	价格	数量
T413821-5mg	5mg	现货
T413821-10mg	10mg	现货
T413821-25mg	25mg	现货
T413821-50mg	50mg	现货
T413821-100mg	100mg	现货

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基本描述

英文别名	TAS-116\|1260533-36-5\|Pimitespib\|Benzamide, 3-ethyl-4-[3-(1-methylethyl)-4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-1H-pyrazolo[3,4-b]pyridin-1-yl]-\|PLO044MUDZ\|3-ethyl-4-[4-[4-(1-methylpyrazol-4-yl)imidazol-1-yl]-3-propan-2-ylpyrazolo[3,4-b]pyridin-
规格或纯度	98%
英文名称	TAS-116
生化机理	TAS-116 is a novel, small-molecule HSP90 inhibitor which inhibits geldanamycin-FITC binding to HSP90 proteins with Ki values of 34.7 nmol/L, 21.3 nmol/L, >50,000 nmol/L, and >50,000 nmol/L for HSP90α, HSP90β, GRP94, and TRAP1, respectively. Furthermore, TAS-116 does not inhibit other ATPases such as HSP70 (IC50 >200 μmol/L).
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	Information TAS-116 TAS-116 is a novel, small-molecule HSP90 inhibitor which inhibits geldanamycin-FITC binding to HSP90 proteins with Ki values of 34.7 nmol/L, 21.3 nmol/L, >50,000 nmol/L, and >50,000 nmol/L for HSP90α, HSP90β, GRP94, and TRAP1, respectively. Furthermore, TAS-116 does not inhibit other ATPases such as HSP70 (IC50 >200 μmol/L). Targets HSP90β (Cell-free assay); HSP90α (Cell-free assay ) 21.3 nM(Ki); 34.7 nM(Ki) In vitro TAS-116 is a selective inhibitor of cytosolic HSP90α and β that does not inhibit HSP90 paralogs such as endoplasmic reticulum GRP94 or mitochondrial TRAP1. Treatment of HCT116 cells with 0.3 μmol/L TAS-116 for 8 hours results in reduced levels of DDR1, which interacts with HSP90α and induction of HSP70, which is a surrogate marker of cytosolic HSP90 inhibition. In vivo Oral administration of TAS-116 leads to tumor shrinkage in human tumor xenograft mouse models accompanied by depletion of multiple HSP90 clients. In a rat model, the antitumor activity of TAS-116 is accompanied by a higher distribution of the compound in subcutaneously xenografted NCI-H1975 non-small cell lung carcinoma tumors than in retina. TAS-116 shows activity against orthotopically transplanted NCI-H1975 lung tumors. Pharmacokinetic profiling of TAS-116 in rodent and nonrodent species shows that TAS-116 is orally absorbed and had a bioavailability of almost 100% in mice, 69.0% in rats, and 73.9% in dogs without special formulation. In a HER2-expressing NCI-N87 human gastric cancer xenograft mouse model, chronic administration of TAS-116 is tolerable, with the average weight loss in mice not exceeding 10% during the treatment period. Cell Research(from reference) Cell lines：HCT116 cells Concentrations：0.3, 1 and 3 μM Incubation Time：8 hours

产品属性

ALogP	3.927
HBD Count	1
Rotatable Bond	6

名称和标识符

IUPAC Name	3-ethyl-4-[4-[4-(1-methylpyrazol-4-yl)imidazol-1-yl]-3-propan-2-ylpyrazolo[3,4-b]pyridin-1-yl]benzamide
INCHI	InChI=1S/C25H26N8O/c1-5-16-10-17(24(26)34)6-7-20(16)33-25-22(23(30-33)15(2)3)21(8-9-27-25)32-13-19(28-14-32)18-11-29-31(4)12-18/h6-15H,5H2,1-4H3,(H2,26,34)
InChi Key	NVVPMZUGELHVMH-UHFFFAOYSA-N
Canonical SMILES	CCC1=C(C=CC(=C1)C(=O)N)N2C3=NC=CC(=C3C(=N2)C(C)C)N4C=C(N=C4)C5=CN(N=C5)C
Isomeric SMILES	CCC1=C(C=CC(=C1)C(=O)N)N2C3=NC=CC(=C3C(=N2)C(C)C)N4C=C(N=C4)C5=CN(N=C5)C
PubChem CID	67501411
分子量	454.53

数据库链接

PubChem CID	67501411
CAS Registry No.	1260533-36-5
ChEMBL Ligand	CHEMBL3661115
DrugBank Ligand	DB14876
BindingDB Ligand	126083

化学和物理性质

溶解性	Solubility (25°C) In vitro DMSO: 91 mg/mL (200.2 mM); Ethanol: 11 mg/mL (24.2 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility	91
DMSO(mM) Max Solubility	200.206807031439
Water(mg / mL) Max Solubility	＜1

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参考文献

1. Suzuki R, Hideshima T, Mimura N, Minami J, Ohguchi H, Kikuchi S, Yoshida Y, Gorgun G, Cirstea D, Cottini F et al.. (2015) Anti-tumor activities of selective HSP90α/β inhibitor, TAS-116, in combination with bortezomib in multiple myeloma.. Leukemia, 29 (2): (510-4). [PMID:25306900]
2. Ohkubo S, Kodama Y, Muraoka H, Hitotsumachi H, Yoshimura C, Kitade M, Hashimoto A, Ito K, Gomori A, Takahashi K et al.. (2015) TAS-116, a highly selective inhibitor of heat shock protein 90α and β, demonstrates potent antitumor activity and minimal ocular toxicity in preclinical models.. Mol Cancer Ther, 14 (1): (14-22). [PMID:25416789]
3. Hoy SM. (2022) Pimitespib: First Approval.. Drugs, 82 (13): (1413-1418). [PMID:35986838]
4. Kawazoe A, Itahashi K, Yamamoto N, Kotani D, Kuboki Y, Taniguchi H, Harano K, Naito Y, Suzuki M, Fukutani M et al.. (2021) TAS-116 (Pimitespib), an Oral HSP90 Inhibitor, in Combination with Nivolumab in Patients with Colorectal Cancer and Other Solid Tumors: An Open-Label, Dose-Finding, and Expansion Phase Ib Trial (EPOC1704).. Clin Cancer Res, 27 (24): (6709-6715). [PMID:34593531]
5. Uno T, Kawai Y, Yamashita S, Oshiumi H, Yoshimura C, Mizutani T, Suzuki T, Chong KT, Shigeno K, Ohkubo M et al.. (2019) Discovery of 3-Ethyl-4-(3-isopropyl-4-(4-(1-methyl-1 H-pyrazol-4-yl)-1 H-imidazol-1-yl)-1 H-pyrazolo[3,4- b]pyridin-1-yl)benzamide (TAS-116) as a Potent, Selective, and Orally Available HSP90 Inhibitor.. J Med Chem, 62 (2): (531-551). [PMID:30525599]
6. Doi T, Kurokawa Y, Sawaki A, Komatsu Y, Ozaka M, Takahashi T, Naito Y, Ohkubo S, Nishida T. (2019) Efficacy and safety of TAS-116, an oral inhibitor of heat shock protein 90, in patients with metastatic or unresectable gastrointestinal stromal tumour refractory to imatinib, sunitinib and regorafenib: a phase II, single-arm trial.. Eur J Cancer, 121 (13): (29-39). [PMID:31536852]

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