2620551-45-1
2620551-45-1 structure
- Name: FLT3-IN-14
- Chemical Name: FLT3-IN-14
- CAS Number: 2620551-45-1
- Molecular Formula: C25H24N6O2S
- Molecular Weight: 472.56
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2022-07-01 07:55:29
- Modify Date: 2024-01-16 18:40:55
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FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model[1].
| Name | FLT3-IN-14 |
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| Description | FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model[1]. |
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| Related Catalog | |
| Target |
IC50: 1.4 nM (FLT-ITD), 5.6 nM (FLT3-WT)[1] |
| In Vitro | FLT3-IN-14 (compound 9c) (0-10 μM; 24 hours) inhibits the proliferation of tested twelve haematological cell lines with IC50s of 0.011-1.582 μM[1]. FLT3-IN-14 (0-10 μM; 72 hours) exhibits low toxicity, with GI50 greater than 10 μM, in resting lymphocytes[1]. FLT3-IN-14 (1-50 nM; 24 and 48 hours) accumulates annexin-V positive cells in a concentration and time-dependent manner[1]. FLT3-IN-14 (25-100 nM; 24 and 48 hours) induces a significant G1 arrest in both cell lines[1]. FLT3-IN-14 (1-50 nM; 24 hours) induces the dephosphorylation of FLT3[1]. Cell Proliferation Assay Cell Line: MOLT-4 , HL-60, KG-1, KG-1a, MOLM-13, MV4-11, NOMO-1, OCI-AML2, PL-21, THP-1, K-562, KCL-22[1] Concentration: 0-10 μM Incubation Time: 24 hours Result: Inhibited the proliferation of these twelve haematological cell lines with IC50s of 0.011-1.582 μM. Cell Cytotoxicity Assay Cell Line: PBL[1] Concentration: 0-10 μM Incubation Time: 72 hours Result: Exhibited low toxicity, with GI50 greater than 10 μM, in resting lymphocytes. Apoptosis Analysis Cell Line: MV4-11[1] Concentration: 1, 10 and 50 nM Incubation Time: 24 and 48 hours Result: Accumulated annexin-V positive cells in a concentration and time-dependent manner. Cell Cycle Analysis Cell Line: MOLM-13 and MV-14[1] Concentration: 25, 50, 75 and 100 nM Incubation Time: 24 and 48 hours Result: Induced a significant G1 arrest in both cell lines. Western Blot Analysis Cell Line: MV-14[1] Concentration: 1, 10 and 50 nM Incubation Time: 24 hours Result: Induced the dephosphorylation of FLT3. |
| In Vivo | FLT3-IN-14 (1.0 and 3.0 mg/kg; IP; daily for 28 days) significantly reduces tumor growth in a dose-dependent manner without sign of toxicity[1]. Animal Model: NOD/SCID female mice (subcutaneously implanted MV4-11)[1] Dosage: 1.0 and 3.0 mg/kg Administration: IP; daily for 28 days Result: Significantly reduced tumor growth by 44.1% and 55.2% at 1 and 3 mg/kg, respectively. |
| References |
| Molecular Formula | C25H24N6O2S |
|---|---|
| Molecular Weight | 472.56 |