中文名称：Adagrasib
英文名称：Adagrasib
CAS No.：2326521-71-3 分子式：C32H35ClFN7O2 分子量：604.1174
产品活性：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。
研究领域：Protein Tyrosine Kinase/RTK
作用靶点：Bcr-Abl
In Vitro: Asciminib (ABL001) hydrochloride binds to the myristoyl pocket of ABL1 and induces the formation of an inactive kinase conformation.
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 BCRABL inhibitor GNF-2 but with approximately 100-fold greater potency.
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.
In BCRABL1-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 BCRABL1 (Tyr245; pBCRABL1) after 1 h using concentrations that correlate with those required for inhibition of cell proliferation.
Asciminib hydrochloride is selectively active against all BCRABL1 lines (IC50 value of 120 nM), irrespective of the presence of either the p210 or the p190 BCRABL1 isoform.
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.
关键字： Asciminib hydrochl;ABL-001 盐酸盐;
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