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  3. Asciminib hydrochloride

Asciminib hydrochloride (Synonyms: ABL001 hydrochloride)

目录号: HY-104010A 纯度: 99.93%
产品使用指南

Asciminib (ABL001) hydrochloride 是一种有效和选择性的变构 BCR-ABL1 抑制剂,抑制 Ba/F3 细胞生长的 IC50 值为 0.25 nM。

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Asciminib hydrochloride Chemical Structure

Asciminib hydrochloride Chemical Structure

CAS No. : 2119669-71-3

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  • 生物活性

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  • 参考文献

生物活性

Asciminib (ABL001) hydrochloride is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM[1].

体外研究
(In Vitro)

Asciminib (ABL001) hydrochloride binds to the myristoyl pocket of ABL1 and induces the formation of an inactive kinase conformation[1].
Asciminib hydrochloride binds potently (dissociation constant=0.5-0.8 nM) and selectively to the myristoyl pocket of ABL1 and induces the inactive C-terminal helix conformation. Asciminib hydrochloride exhibits the same non-ATP-competitive biochemical kinetics as the BCR–ABL inhibitor GNF-2 but with approximately 100-fold greater potency[1].
Asciminib hydrochloride lacks activity against more than 60 kinases, including SRC, and is similarly inactive against G-protein-coupled receptors, ion channels, nuclear receptors and transporters[1].
In BCR–ABL1-transformed Ba/F3 cells grown without IL-3, Asciminib hydrochloride has an anti-proliferative with IC50 value of 0.25 nM. In the CML blast-phase cell line KCL-22, Asciminib hydrochloride inhibits phosphorylation of both STAT5 (Tyr694; pSTAT5) and BCR–ABL1 (Tyr245; pBCR–ABL1) after 1 h using concentrations that correlate with those required for inhibition of cell proliferation[1].
Asciminib hydrochloride is selectively active against all BCR–ABL1 lines (IC50 value of 1–20 nM), irrespective of the presence of either the p210 or the p190 BCR–ABL1 isoform[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Single doses of 7.5, 15 and 30 mg/kg Asciminib, administered to mice bearing KCL- 22 xenografts, inhibits pSTAT5 (Tyr694), which return to baseline at 10, 12 and 16-20 h after administration of the dose, respectively. In mice implanted with KCL-22 tumors, the minimum dose of Asciminib required for complete regression is 7.5 mg/kg twice a day (BID) or 30 mg/kg once a day (QD), and is tolerated at doses up to 250 mg/kg BID[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

486.30

Formula

C20H19Cl2F2N5O3

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献
Cell Assay

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
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产品名称:
Asciminib hydrochloride
目录号:
HY-104010A
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