[CAS NO. 847928-32-9] 1G244

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PRODUCTS SPECIFICATIONS [847928-32-9]

Catalog

HY-116304

Brand

MCE

CAS

847928-32-9

DESCRIPTION [847928-32-9]

Overview

MDL	MFCD28167087
Molecular Weight	504.57
Molecular Formula	C29H30F2N4O2
SMILES	O=C(N1CC2=C(C=CC=C2)C1)[C@@H](N)CC(N3CCN(C(C4=CC=C(F)C=C4)C5=CC=C(F)C=C5)CC3)=O

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

1 Publications Citing Use of MCE

[1]Nat Chem Biol. 2022 Nov 10.

Summary

1G244 is a potent DPP8/9 inhibitor with IC ₅₀ s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects ^[1] ^[2] .

IC50 & Target

IC50: 12 nM (DPP8), 84 nM (DPP9) ^[2]

In Vitro

1G244 (0-100 μM; 72 hours; Delta47, U266 , KMS-5, RPMI8226, or MM.1 S cells) treatment dose-dependently decreases viable cell number of five multiple myeloma cell lines ^[1] .
1G244 (50 μM; 0-48 hours; MM.1 S cells) treatment induces apoptosis, as cleaved forms of both caspase-3 and PARP are detected ^[1] .

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

Cell Viability Assay ^[1]

Cell Line:	Delta47, U266 , KMS-5, RPMI8226, or MM.1 S cells
Concentration:	0 μM, 1 μM, 5 μM, 10 μM, 50 μM, or 100 μM
Incubation Time:	72 hours
Result:	Dose-dependently decreased viable cell number of five multiple myeloma cell lines.

Western Blot Analysis ^[1]

Cell Line:	MM.1 S cells
Concentration:	50 μM
Incubation Time:	0 hour, 3 hours, 6 hours, 12 hours, 24 hours, 48 hours
Result:	Decreased caspase-3 and PARP protein.

In Vivo

1G244 (30 mg/kg; subcutaneous injection; once-a-week; for 3 weeks; NOG female mice) treatment apparently suppresses the subcutaneous growth of MM.1 S cells in murine xenograft model ^[1] .

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

Animal Model:	NOD/Shi-scid IL-2Rγnull (NOG) female mice (6-7 weeks; 19-21 g) injected with MM.1 S cells ^[1]
Dosage:	30 mg/kg
Administration:	Subcutaneous injection; once-a-week; for 3 weeks
Result:	Apparently suppressed the subcutaneous growth of MM.1 S cells in murine xenograft model.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

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

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL ( 495.47 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9819 mL	9.9094 mL	19.8189 mL
5 mM	0.3964 mL	1.9819 mL	3.9638 mL
10 mM	0.1982 mL	0.9909 mL	1.9819 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 (4.12 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.12 mM); Clear solution

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