Pulrodemstat(Synonyms: CC-90011; LSD1-IN-7)

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Pulrodemstat (Synonyms: CC-90011; LSD1-IN-7)

Pulrodemstat (CC-90011) 是一种有效的，选择性的，可逆的和具有口服活性的赖氨酸特异性脱甲基酶-1 (LSD1) 抑制剂，IC50 为 0.25 nM。Pulrodemstat 对 LSD2，MOA-A 和 MAO-B 的酶抑制作用较小。Pulrodemstat 诱导急性髓细胞性白血病 (AML)和小细胞肺癌 (SCLC) 细胞分化，并具有有效的抗癌活性。

Pulrodemstat(Synonyms: CC-90011; LSD1-IN-7)

Pulrodemstat Chemical Structure

CAS No. : 1821307-10-1

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Pulrodemstat 的其他形式现货产品:

Pulrodemstat benzenesulfonate

生物活性

Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity[1].

IC50 & Target

IC50: 0.25 nM (LSD1)[1]
体外研究
(In Vitro)

Pulrodemstat (CC-90011, Compound 11) shows potent induction of on-target cellular differentiation marker CD11b in THP-1 cell line with an EC50 of 7 nM, antiproliferative activity in AML kasumi-1 cells with an EC50 of 2 nM[1].
Suppression of GRP is observed with treatment of Pulrodemstat (4 days) in a dose-dependent manner and at pharmacologically useful concentrations (EC50=3 nM, H209 and 4 nM, H1417). Pulrodemstat (12 days) treatment of SCLC cells results in potent antiproliferative activity (EC50=6 nM, H1417) that correlated with GRP suppression[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Pulrodemstat (CC-90011; 5 mg/kg; oral administration; daily; for 30 days; for 30 days) treatment inhibits tumor growth in patient-derived xenograft SCLC models[1].
Pulrodemstat (once a day; for 4 days) treatment results in robust downregulation of GRP mRNA levels at 2.5 mg/kg and maximum suppression of GRP at 5 mg/kg in a SCLC human tumor xenograft (H1417) mice[1].
After i.v. administration, Pulrodemstat (Compound 11; 5 mg/kg) has systemic clearance of 32.4 mL/min/kg, elimination half-life of 2 h, and a high volume of distribution of 7.5 L/kg. Pulrodemstat (Compound 11; 5 mg/kg) is readily absorbed after oral administration with an AUC0-24h of 1.8 μM·h, C/sub>max of 0.36 μM, and oral bioavailability of 32%[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude mice bearing small cell lung carcinoma (SCLC)[1]
Dosage: 5 mg/kg
Administration: Oral administration; daily; for 30 days
Result: Showed a tumor growth inhibition (TGI) of 78% at 5 mg/kg with no body weight loss.

分子量

451.47

Formula

C24H23F2N5O2
CAS 号

1821307-10-1
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.
参考文献

  • [1]. Toufike Kanouni, et al. Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1). J Med Chem. 2020 Dec 10;63(23):14522-14529.

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