GDC-0575 2HCl

This product is for research use only, not for human use. We do not sell to patients.

GDC-0575 2HCl
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Cat #: V3691 CAS #: 1657014-42-0 (2HCl salt) Purity ≥ 98%

Description: GDC-0575 (also called ARRY-575, RG7741) is a novel, potent and selective inhibitor of CHK1 (Check point kinases) which specifically binds to and inhibits CHK1 with an IC50 of 1.2 nM.

References: Di Tullio A, et al. The combination of CHK1 inhibitor with G-CSF overrides cytarabine resistance in human acute myeloid leukemia. Nat Commun. 2017 Nov 22;8(1):1679.

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Molecular Weight (MW)451.19
Molecular FormulaC16H22BrCl2N5O
CAS No.1657014-42-0 (2HCl salt)
Storage-20℃ for 3 years in powder formrr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: >100 mg/mLrr
Water:rr
Ethanol:
SynonymsARRY-575 2HCl; ARRY-575; ARRY575; RG7741; RG-7741 2HCl; RG 7741; GDC-0575; GDC 0575 2HCl; GDC0575; AK 687476 2HCl; AK-687476; AK687476 dihydrochloric acid
ProtocolIn VitroGDC-0575 dihydrochloride is a selective and orally bioavailable CHK1 inhibitor, with an IC50 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)
In VivoGDC-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
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.2164 mL11.0818 mL22.1636 mL44.3272 mL
5mM0.4433 mL2.2164 mL4.4327 mL8.8654 mL
10mM0.2216 mL1.1082 mL2.2164 mL4.4327 mL
20mM0.1108 mL0.5541 mL1.1082 mL2.2164 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
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Volume
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Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
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Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.