1. Epigenetics
  2. Histone Demethylase
  3. Pulrodemstat benzenesulfonate

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

Cat. No.: HY-129388B Purity: 99.39%
Handling Instructions

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

For research use only. We do not sell to patients.

Pulrodemstat benzenesulfonate Chemical Structure

Pulrodemstat benzenesulfonate Chemical Structure

CAS No. : 2097523-60-7

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Solution
10 mM * 1 mL in DMSO USD 221 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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5 mg USD 165 In-stock
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10 mg USD 275 In-stock
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50 mg USD 935 In-stock
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100 mg USD 1595 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

Other Forms of Pulrodemstat benzenesulfonate:

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1 Publications Citing Use of MCE Pulrodemstat benzenesulfonate

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  • References

  • Customer Review

Description

CC-90011 benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 benzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 benzenesulfonate 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]

In Vitro

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 CC-90011 (4 days) in a dose-dependent manner and at pharmacologically useful concentrations (EC50=3 nM, H209 and 4 nM, H1417). CC-90011 (12 days) treatment of SCLC cells results in potent antiproliferative activity (EC50=6 nM, H1417) that correlated with GRP suppression[1].

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

In Vivo

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].
CC-90011 (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, CC-90011 (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. CC-90011 (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].

MCE 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.
Clinical Trial
Molecular Weight

609.64

Formula

C30H29F2N5O5S

CAS No.
SMILES

N#CC1=CC=C(C(N=C(N2CCC(N)CC2)N3C)=C(C4=CC=C(OC)C(F)=C4)C3=O)C=C1F.O=S(C5=CC=CC=C5)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (82.02 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6403 mL 8.2016 mL 16.4031 mL
5 mM 0.3281 mL 1.6403 mL 3.2806 mL
10 mM 0.1640 mL 0.8202 mL 1.6403 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.41 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.41 mM); Clear solution

*All of the co-solvents are available by MCE.
References

Purity: 99.39%

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Pulrodemstat benzenesulfonate
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