2. Immunology/Inflammation
  3. PD-1/PD-L1
  4. SCL-1

SCL-1 is an orally active anti-PD-1/PD-L1 inhibitor. SCL-1 can inhibit PD-1/PD-L1 binding. SCL-1 increases T cells, B cells and natural killer cells. SCL-1 exerts strong tumor growth inhibitory effects that were mediated by effector T-cell induction inside tumors and the up-regulated expression of long non-coding RNAs as neoantigens leading to cytotoxic T lymphocyte activation. SCL-1 can be used for the research of cancer, such as triple-negative breast cancer.

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SCL-1

SCL-1 Chemische Struktur

CAS. Nr. : 1061105-16-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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SCL-1 Related Antibodies

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Beschreibung

SCL-1 is an orally active anti-PD-1/PD-L1 inhibitor. SCL-1 can inhibit PD-1/PD-L1 binding. SCL-1 increases T cells, B cells and natural killer cells. SCL-1 exerts strong tumor growth inhibitory effects that were mediated by effector T-cell induction inside tumors and the up-regulated expression of long non-coding RNAs as neoantigens leading to cytotoxic T lymphocyte activation. SCL-1 can be used for the research of cancer, such as triple-negative breast cancer[1][2].

In Vitro

SCL-1 (0.25-100 μM, 4 days) has no significant cytotoxicity in MDA-MB231 cell[1].
SCL-1 (25 μM) inhibits exhibits moderate inhibitory activities against PD-1/PD-L1 binding with inhibition rate of 63%[2].
SCL-1 inhibits SCC3 and Jurkat cell proliferation with IC50 values >50 μM[2].

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

SCL-1 Related Antibodies
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax
Mice[1] 100 mg/kg p.o. 1.75 h 0.5 h 4.63 μg/mL
In Vivo

SCL-1 (25-100 mg/kg, p.o., 10 times over 14 days) inhibits tumor growth in humanized MDA-MB231 tumor tumor-bearing MHC-dKO NOG mice[1].
SCL-1 (50 mg/kg, p.o., 10 times over 14 days) suppresses tumor growth in humanized SCC-3 tumor-bearing MHC-dKO NOG mice[2].

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

Animal Model: MDA-MB231 tumor in a humanized MHC-double knockout NOG mice models[1]
Dosage: 25, 50 and 100 mg/kg
Administration: Orally administered, 10 times over 14 days (days 1-5 and 8-12)
Result: Inhibited tumor volume.
Did not induce weight loss.
Increased infiltrated CD4+ and CD8+ T-cell numbers inside tumors.
Increased the frequency of CD19+ B cells that infiltrated tumors.
Showed high level of lymphoid cell infiltration.
Upregulated T cell-associated cytotoxic genes (GZMB, PRF1, and IFNB1), exhausted marker genes (PD-1, TIM3, and CD39), NK activation-associated genes (CD16 and NCR1), and T-cell attracting chemokine genes (CCL3 and CCL4).
Downregulated CXCL12 gene expression.
Upregulated tumor-specific long non-coding (lnc) RNAs.
Animal Model: Humanized SCC-3 tumor-bearing MHC-dKO NOG mice[2]
Dosage: 50 mg/kg
Administration: Orally administered, 10 times over 14 days (days 1-5 and 8-12)
Result: Promoted the engraftment of transplanted human PBMCs in the spleens.
Increased the number of infiltrated CD45+ human PBMCs and CD4+ and CD8+ T cells inside the tumors.
Had more foci of lymphoid cell infiltration with necrotic changes.
Increased CD8+ T cells.
Upregulated the expression of CXCL9 and CXCR3.
Downregulated the expression levels of CCL22 and TIM3.
Molekulargewicht

396.41

Formel

C18H23F3N6O
CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

CC1CCCCN1C(C2CCN(CC2)C3=NN4C(C=C3)=NN=C4C(F)(F)F)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 100 mg/mL (252.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5226 mL 12.6132 mL 25.2264 mL
5 mM 0.5045 mL 2.5226 mL 5.0453 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molaritätsrechner

  • Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.5 mg/mL (6.31 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (6.31 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
Verweise

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5226 mL 12.6132 mL 25.2264 mL 63.0660 mL
5 mM 0.5045 mL 2.5226 mL 5.0453 mL 12.6132 mL
10 mM 0.2523 mL 1.2613 mL 2.5226 mL 6.3066 mL
15 mM 0.1682 mL 0.8409 mL 1.6818 mL 4.2044 mL
20 mM 0.1261 mL 0.6307 mL 1.2613 mL 3.1533 mL
25 mM 0.1009 mL 0.5045 mL 1.0091 mL 2.5226 mL
30 mM 0.0841 mL 0.4204 mL 0.8409 mL 2.1022 mL
40 mM 0.0631 mL 0.3153 mL 0.6307 mL 1.5767 mL
50 mM 0.0505 mL 0.2523 mL 0.5045 mL 1.2613 mL
60 mM 0.0420 mL 0.2102 mL 0.4204 mL 1.0511 mL
80 mM 0.0315 mL 0.1577 mL 0.3153 mL 0.7883 mL
100 mM 0.0252 mL 0.1261 mL 0.2523 mL 0.6307 mL
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SCL-1 Related Classifications

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:

SCL-11061105-16-5SCL1SCL 1PD-1/PD-L1PD-1/Programmed death-ligand 1PD-1PD-L1T cellsB cellsNk cellsCTLMDA-MB231SCC3MHCInhibitorinhibitorinhibit

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