2. Metabolic Enzyme/Protease
  3. Dihydroorotate Dehydrogenase
  4. DHODH-IN-22

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)。

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DHODH-IN-22 Chemical Structure

DHODH-IN-22 Chemical Structure

CAS No. : 2450341-75-8

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DHODH-IN-22 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DHODH-IN-22 is a potent, selective and orally active dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 value 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]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MOLM-13 IC50
0.4 nM
Compound: 29
Antiproliferative activity against human MOLM-13 cells incubated for 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human MOLM-13 cells incubated for 72 hrs by CellTiter-Glo assay
[PMID: 35925768]
THP-1 IC50
1.4 nM
Compound: 29
Antiproliferative activity against human THP-1 cells assessed as reduction in cell viability measured after 72 hrs
Antiproliferative activity against human THP-1 cells assessed as reduction in cell viability measured after 72 hrs
[PMID: 35925768]
体外研究
(In Vitro)

DHODH-IN-22 (compound 29) exhibits antiproliferative activity against MOLM-13 and THP-1 cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

DHODH-IN-22 相关抗体:

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.
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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female NSG mice (implanted subcutaneously with 2 × 106 MOLM-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.
分子量

548.88

Formula

C21H21ClF4N6O5
CAS 号
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.
纯度 & 产品资料
参考文献

DHODH-IN-22 相关分类

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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DHODH-IN-222450341-75-8Dihydroorotate DehydrogenaseDHODHacute myelogenous leukemiaAMLMOLM-13THP-1antiproliferativeNSG miceantitumorInhibitorinhibitorinhibit

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