FLT3-IN-1
Modify Date: 2024-01-02 13:33:28
FLT3-IN-1 structure
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Common Name | FLT3-IN-1 | ||
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| CAS Number | 1370256-78-2 | Molecular Weight | 537.65700 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C25H27N7O3S2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of FLT3-IN-1SKLB4771 is a novel potent and selective Flt3 inhibitor with IC50 of 10 nM; against FLT3-ITD-expressing MV4-11 cells with IC50 of 6 nM.IC50 value: 10 nM (in vitro) [1]Target: in vitro: SKLB4771 inhibited FLT3 phosphorylation in a dose-dependent manner. Consistent with the downregulation of the phosphorylation of FLT3, the phosphorylation of the downstream signaling proteins STAT5 and ERK1/2 was also significantly inhibited at concentrations >0.1 μM. SKLB4771 potently inhibited the growth of MV4-11 cells that express FLT3-ITD, with an IC50 value of 0.006 μM. It just exhibited very weak inhibitory activity against human T lymphoma Jurkat cells, human Burkitt's lymphoma Ramos cells, human lung cancer PC-9 and H292 cells, and human epithelial carcinoma A431 cells (IC50: 3.05 μM, 6.25 μM, 3.72 μM, 6.94 μM, and 8.91 μM, respectively). For other leukemia and solid tumor cell lines, including K562, U937, Karpas299, HCC827, A549, H2228, H820, MDA-MB-231, BT474, MCF-7, HCT116, SW480, LoVo, HeLa, SKOV-3, SK, DU145, PC-3, A431, and SH-SY5Y [1].in vivo: Treatment with SKLB4771 at 100 mg/kg/d resulted in rapid and complete tumor regression in all mice of this group. SKLB4771 treatment at 20 mg/kg/d and 40 mg/kg/d significantly slowed down the tumor growth; the tumor inhibition rates are 66% and 84%, respectively. Moreover, during the whole experiment, no significant weight loss or any other obvious signs of toxicity were observed for all of the SKLB4771 treated mice. |
| Name | 1-{5-[7-(3-morpholinopropoxy)quinazolin-4-ylthio][1,3,4]thiadiazol-2-yl}-3-p-tolylurea |
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| Synonym | More Synonyms |
| Description | SKLB4771 is a novel potent and selective Flt3 inhibitor with IC50 of 10 nM; against FLT3-ITD-expressing MV4-11 cells with IC50 of 6 nM.IC50 value: 10 nM (in vitro) [1]Target: in vitro: SKLB4771 inhibited FLT3 phosphorylation in a dose-dependent manner. Consistent with the downregulation of the phosphorylation of FLT3, the phosphorylation of the downstream signaling proteins STAT5 and ERK1/2 was also significantly inhibited at concentrations >0.1 μM. SKLB4771 potently inhibited the growth of MV4-11 cells that express FLT3-ITD, with an IC50 value of 0.006 μM. It just exhibited very weak inhibitory activity against human T lymphoma Jurkat cells, human Burkitt's lymphoma Ramos cells, human lung cancer PC-9 and H292 cells, and human epithelial carcinoma A431 cells (IC50: 3.05 μM, 6.25 μM, 3.72 μM, 6.94 μM, and 8.91 μM, respectively). For other leukemia and solid tumor cell lines, including K562, U937, Karpas299, HCC827, A549, H2228, H820, MDA-MB-231, BT474, MCF-7, HCT116, SW480, LoVo, HeLa, SKOV-3, SK, DU145, PC-3, A431, and SH-SY5Y [1].in vivo: Treatment with SKLB4771 at 100 mg/kg/d resulted in rapid and complete tumor regression in all mice of this group. SKLB4771 treatment at 20 mg/kg/d and 40 mg/kg/d significantly slowed down the tumor growth; the tumor inhibition rates are 66% and 84%, respectively. Moreover, during the whole experiment, no significant weight loss or any other obvious signs of toxicity were observed for all of the SKLB4771 treated mice. |
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| Related Catalog | |
| References |
| Molecular Formula | C25H27N7O3S2 |
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| Molecular Weight | 537.65700 |
| Exact Mass | 537.16200 |
| PSA | 167.93000 |
| LogP | 4.76990 |
| Appearance of Characters | white solid |
| Storage condition | -20℃ |
| 1-(5-(7-(3-morpholinopropoxy)quinazolin-4-ylthio)-1,3,4-thiadiazol-2-yl)-3-p-tolylurea |
| FLT3-IN-1 |
| SKLB4771 |