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ABBV-167 Sale

目录号 : GC64674

ABBV-167 是一种 BCL-2 抑制剂 venetoclax 的磷酸盐前药。

ABBV-167 Chemical Structure

Cas No.:1351456-78-4

规格 价格 库存 购买数量
5 mg
¥3,600.00
现货
10 mg
¥6,120.00
现货
25 mg
¥12,150.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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产品描述

ABBV-167 is a phosphate prodrug of the BCL-2 inhibitor venetoclax.

[1]. Salem AH, et al. Expanding the Repertoire for "Large Small Molecules": Prodrug ABBV-167 Efficiently Converts to Venetoclax with Reduced Food Effect in Healthy Volunteers. Mol Cancer Ther. 2021 Jun;20(6):999-1008.

Chemical Properties

Cas No. 1351456-78-4 SDF Download SDF
分子式 C46H53ClN7O11PS 分子量 978.45
溶解度 DMSO : 100 mg/mL (102.20 mM; Need ultrasonic) 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.022 mL 5.1101 mL 10.2202 mL
5 mM 0.2044 mL 1.022 mL 2.044 mL
10 mM 0.1022 mL 0.511 mL 1.022 mL
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Research Update

Expanding the Repertoire for "Large Small Molecules": Prodrug ABBV-167 Efficiently Converts to Venetoclax with Reduced Food Effect in Healthy Volunteers

Mol Cancer Ther 2021 Jun;20(6):999-1008.PMID:33785651DOI:10.1158/1535-7163.MCT-21-0077

Since gaining approval for the treatment of chronic lymphocytic leukemia (CLL), the BCL-2 inhibitor venetoclax has transformed the treatment of this and other blood-related cancers. Reflecting the large and hydrophobic BH3-binding groove within BCL-2, venetoclax has significantly higher molecular weight and lipophilicity than most orally administered drugs, along with negligible water solubility. Although a technology-enabled formulation successfully achieves oral absorption in humans, venetoclax tablets have limited drug loading and therefore can present a substantial pill burden for patients in high-dose indications. We therefore generated a phosphate prodrug (3, ABBV-167) that confers significantly increased water solubility to venetoclax and, upon oral administration to healthy volunteers either as a solution or high drug-load immediate release tablet, extensively converts to the parent drug. Additionally, ABBV-167 demonstrated a lower food effect with respect to venetoclax tablets. These data indicate that beyond-rule-of-5 molecules can be successfully delivered to humans via a solubility-enhancing prodrug moiety to afford robust exposures of the parent drug following oral dosing.