DHODH-IN-22 是一种有效且具有选择性和口服活性的二氢乳清酸脱氢酶 (DHODH) 抑制剂，IC50为 0.3 nM。DHODH-IN-22可用于研究急性髓系白血病 (AML)。
| 生物活性 | DHODH-IN-22 is a potent, selective and orally activedihydroorotate dehydrogenase(DHODH)inhibitor with anIC50value of 0.3 nM. DHODH-IN-22 can be used for researching acute myelogenous leukemia (AML)[1]. |
| IC50& Target | IC50: 0.3 nM (human DHODH), 10 nM (mouse DHODH), 130 nM (rat DHODH), 4.2 nM (dog DHODH), 0.54 nM (monkey DHODH)[1] |
体外研究
(In Vitro) | DHODH-IN-22 (compound 29) exhibits antiproliferative activity against MOLM-13 and THP-1 cells[1].
Cell Proliferation Assay[1] | Cell Line: | MOLM-13 and THP-1 | | Concentration: | 0-30 nM | | Incubation Time: | 72 h | | Result: | Exhibited antiproliferative activity against MOLM-13 and THP-1 cells with IC50s of 0.4 nM and 1.4 nM, respectively. |
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体内研究
(In Vivo) | DHODH-IN-22 (1.9-7.5 mg/kg; PO; QD for 5 days) significantly inhibits MOLM-13 tumor growth in mice, and exhibits no significant impact on body weight[1].
DHODH-IN-22 (2 mg/kg for IV and 10 mg/kg for PO; single dosage) has favorable pharmacokinetic property[1].
Pharmacokinetic Parameters of DHODH-IN-22 (compound 29) in mouse and rat[1].
| Mouse
IV 2 mg/kg and PO 10 mg/kg | Rat
IV 2 mg/kg and PO 10 mg/kg | | CL (mL/min/kg) | 7.3 | 7.6 | | Vdss(L/kg) | 2.4 | 2.2 | | t1/2(ng/mL) | 5 | 4 | | Cmax(ng/mL) | 3810 | 2193 | | tmax(h) | 1.0 | 4.0 | | AUC0-inf(ng/mL·h) | 23046 | 23807 | | F (%) | 110 | 106 |
| Animal Model: | Female NSG mice (implanted subcutaneously with 2 × 106MOLM-13 tumor cells)[1] | | Dosage: | 1.9, 3.75 and 7.5 mg/kg | | Administration: | PO; QD for 5 days | | Result: | Significantly inhibited tumor growth with ΔTGI% of 71, 76, and 79% at 1.9, 3.75 and 7.5 mg/kg, respectively, and exhibited no significant impact on body weight over the course of 5 days. |
| Animal Model: | Rat and mouse[1] | | Dosage: | 2 mg/kg IV and 10 mg/kg PO | | Administration: | IV or PO; single dosage (Pharmacokinetic analysis) | | Result: | Exhibited low clearance and high oral bioavailability in both species. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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