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GDC-0834 Racemate Sale

(Synonyms: N-[3-[6-[[4-(1,4-二甲基-3-氧代-2-哌嗪基)苯基]氨基]-4,5-二氢-4-甲基-5-氧代-2-吡嗪基]-2-甲基苯基]-4,5,6,7-四氢苯并[B]噻吩-2-甲酰胺) 目录号 : GC36127

GDC-0834 Racemate 是 GDC-0834 的外消旋体形式,它是一种有效的选择性 BTK 抑制剂,在生化和细胞试验中的体外 IC50 分别为 5.9 和 6.4 nM。

GDC-0834 Racemate Chemical Structure

Cas No.:1133432-46-8

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥2,127.00
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2mg
¥1,060.00
现货
5mg
¥1,620.00
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10mg
¥2,412.00
现货
50mg
¥7,254.00
现货
100mg 待询 待询
200mg 待询 待询

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Sample solution is provided at 25 µL, 10mM.

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产品描述

GDC-0834 Racemate is the racemate form of GDC-0834, which is a potent and selective BTK inhibitor with in vitro IC50s of 5.9 and 6.4 nM in biochemical and cellular assays, respectively.IC50 value: 5.9 nM/6.4 nM(biochemical/cellular assay) [1]Target: BTKin vitro: GDC-0834 inhibited BTK with an in vitro IC(50) of 5.9 and 6.4 nM in biochemical and cellular assays, respectively, and in vivo IC(50) of 1.1 and 5.6 μM in mouse and rat, respectively [1].in vivo: Administration of GDC-0834 (30-100 mg/kg) in a rat collagen-induced arthritis (CIA) model resulted in a dose-dependent decrease of ankle swelling and reduction of morphologic pathology [1]. GDC-0834 exhibited low clearance in PXB chimeric mice with humanized liver. Uncertainty in human pharmacokinetic prediction and high interest in a BTK inhibitor for clinical evaluation prompted an investigational new drug strategy, in which GDC-0834 was rapidly advanced to a single-dose human clinical trial. GDC-0834 plasma concentrations in humans were below the limit of quantitation (<1 ng/ml) in most samples from the cohorts dosed orally at 35 and 105 mg [2].

[1]. Liu L, et al. Antiarthritis effect of a novel Bruton's tyrosine kinase (BTK) inhibitor in rat collagen-induced arthritis and mechanism-based pharmacokinetic/pharmacodynamic modeling: relationships between inhibition of BTK phosphorylation and efficacy. J Pharmacol Exp Ther. 2011 Jul;338(1):154-63. [2]. Liu L, et al. Significant species difference in amide hydrolysis of GDC-0834, a novel potent and selective Bruton's tyrosine kinase inhibitor. Drug Metab Dispos. 2011 Oct;39(10):1840-9.

Chemical Properties

Cas No. 1133432-46-8 SDF
别名 N-[3-[6-[[4-(1,4-二甲基-3-氧代-2-哌嗪基)苯基]氨基]-4,5-二氢-4-甲基-5-氧代-2-吡嗪基]-2-甲基苯基]-4,5,6,7-四氢苯并[B]噻吩-2-甲酰胺
Canonical SMILES O=C(C1=CC(CCCC2)=C2S1)NC3=CC=CC(C(N=C4NC5=CC=C(C6N(C)CCN(C)C6=O)C=C5)=CN(C)C4=O)=C3C
分子式 C33H36N6O3S 分子量 596.74
溶解度 DMSO: ≥ 49 mg/mL (82.11 mM) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 1.6758 mL 8.3789 mL 16.7577 mL
5 mM 0.3352 mL 1.6758 mL 3.3515 mL
10 mM 0.1676 mL 0.8379 mL 1.6758 mL
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