[CAS NO. 1657014-42-0] GDC-0575dihydrochloride

Name: GDC-0575dihydrochloride
Brand: Arctom Scientific
SKU: AS948122

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PRODUCTS SPECIFICATIONS [1657014-42-0]

Distributor

Catalog

AS948122

Brand

Arctom Scientific

CAS

1657014-42-0

DESCRIPTION [1657014-42-0]

Overview

MDL	-
Molecular Weight	451.19
Molecular Formula	C16H22BrCl2N5O
SMILES	O=C(C1CC1)NC2=CNC3=NC=C(Br)C(N4C[C@H](N)CCC4)=C32.[H]Cl.[H]Cl

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

4 Publications Citing Use of MCE

Summary

GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) is an orally bioavailable CHK1 inhibitor, with an IC ₅₀ of 1.2 nM, and has antitumor activity.

IC50 & Target

Chk1

1.2 nM (IC ₅₀ )

In Vitro

GDC-0575 dihydrochloride is a selective and orally bioavailable CHK1 inhibitor, with an IC ₅₀ of 1.2 nM. GDC-0575 (100 nM) suppressses CHK1 activation induced by AraC by decreasing the level of Tyr15-phosphorylated CDK2. GDC-0575 (100 nM) has no effect on the viability of AML cells, but significantly reduces cell viability and induces apoptosis in combination with AraC. In addition, GDC-0575 plus AraC shows no effect on normal hematopoietic stem and progenitor cells (HSPCs) ^[1] . GDC-0575 shows cytotoxic activity against most of 20 melanoma cell lines tested, but several cell lines grown as tumour sphere (TS) are relatively insensitive ^[2] .

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

In Vivo

GDC-0575 (7.5 mg/kg, p.o.) in combination with AraC alomost completely eradicates leukemic burden in mice transplanted with U937-Luc cells, and shows more efficient activity than AraC alone. Furthermore, GDC-0575 elevates the cytotoxicity of AraC in different primary AML models in vivo ^[1] . GDC-0575 (25, 50 mg/kg, p.o.) dose-dependently inhibits the growth of tumor in D20 and C002 xenografts ^[2] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01564251	Genentech, Inc.	Lymphoma, Solid Tumor	March 23, 2012	Phase 1

Appearance

Solid

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 : 65 mg/mL ( 144.06 mM ; Need ultrasonic)

H ₂ O : 25 mg/mL ( 55.41 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2164 mL	11.0818 mL	22.1636 mL
5 mM	0.4433 mL	2.2164 mL	4.4327 mL
10 mM	0.2216 mL	1.1082 mL	2.2164 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS

Solubility: 10 mg/mL (22.16 mM); Clear solution; Need ultrasonic
2.

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

Solubility: ≥ 2.17 mg/mL (4.81 mM); Clear solution
3.

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

Solubility: ≥ 2.17 mg/mL (4.81 mM); Clear solution
4.

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

Solubility: ≥ 2.17 mg/mL (4.81 mM); Clear solution

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

References

Synonyms

Cyclopropanecarboxamide, N-[4-[(3R)-3-amino-1-piperidinyl]-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl]-, hydrochloride (1:2)