Lasmotinib
CAS No. : 2127107-15-5
(Synonyms: PHI-101)
| Size | Price | Stock |
|---|---|---|
| 1mg | $100 | In-stock |
| 5mg | $200 | In-stock |
| 10mg | $360 | In-stock |
| 25mg | $830 | In-stock |
| 50mg | $1500 | In-stock |
| 100mg | $2700 | In-stock |
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| Cat. No. : | HY-153857 |
| M.Wt: | 386.44 |
| Formula: | C19H19FN4O2S |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic) |
Lasmotinib (PHI-101) is a FLT3 and CHK2 inhibitor. Lasmotinib potently inhibits FLT3 single activating mutations (ITD or TKD mutants) and has inhibitory activity against FLT3 double (ITD/D835Y or ITD/F691L) and triple (ITD/D835Y/F691L) resistance mutations. Lasmotinib synergizes with Venetoclax (HY-15531) or Azacytidine to inhibit leukemia. Lasmotinib exhibits anticancer activity against ovarian and breast cancer[1][2][3][4].
In Vitro:Lasmotinib (PHI-101) 是一种 FLT3 和 CHK2 抑制剂。Lasmotinib 有效抑制 FLT3 单激活突变 (ITD 或 TKD 突变体)，并对 FLT3 双 (ITD/D835Y 或 ITD/F691L) 和三 (ITD/D835Y/F691L) 耐药突变 具有抑制活性。Lasmotinib 与 Venetoclax (HY-15531) 或 Azacytidine 协同抑制白血病。Lasmotinib 对卵巢癌和乳腺癌表现出抗癌活性[1][2][3][4]。
In Vivo:Lasmotinib 抑制 FLT3 突变细胞 MV4-11、Molm13 和 Molm14 的生长，GI50 值分别为 7.0 nM、3.8 nM 和 3.4 nM[2]。
Lasmotinib (72 h) 与 PARP1 抑制剂 Olaparib (HY-10162) 联合治疗卵巢癌细胞和乳腺癌细胞无论细胞中是否存在功能性 BRCA 和 P53 都引发协同致死反应[3]。
Lasmotinib 对难治性卵巢癌细胞和乳腺癌细胞表现出抗癌活性[3]。
Lasmotinib 与 Venetoclax (HY-15531) 或 Azacytidine 联合治疗对 FLT3-ITD 突变型和野生型 AML 细胞生长抑制表现出强大的协同作用[4]。
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