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GDC-0575

CAT: 0013-GTR19164339-01Size: 200 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19164339-01Size:200 mg
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Description
GDC-0575 (ARRY-575, RG-7741) is a potent, selective and orally bioavailable Chk1 inhibitor with IC50 of 1.2 nM; enhances the killing of primary AML cells ex vivo by inducing apoptosis combined with AraC, blocks the activation of CHK1 induced by AraC via decrease in the level of Tyr15-phosphorylated CDK2 at 100 nM in AML cells.Blood Cancer Phase 1 Clinical (In Vitro) :GDC-0575 is significantly more potent in promoting DNA damage, replication stress and cell death than V158411, LY2603618, and MK-8776 in a panel of melanoma cell lines. GDC-0575 abrogates DNA damage-induced S and G2–M checkpoints, exacerbates DNA double-strand breaks and induces apoptosis in STS cells. GDC-0575 has a synergistic or additive effect together with gemcitabine. CHK1 inhibitor GDC-0575 in combination with AraC enhances the killing of primary acute myeloid leukemia cells ex vivo by inducing apoptosis. (In Vivo) :GDC-0575 is active at 25 mg/kg as a single agent, but the efficacy is improved at the higher drug dose. GDC-0575 effectively blocks tumor growth in the D20 and C002 xenografts, and the effect is maintained for at least 10 days after the final dose is administered.
CAS Number
1196541-47-5
Product Name Alternative
ARRY-575 | RG-7741 | GDC0575
Purity
>98% (HPLC)
Solubility
DMSO : ≥ 50 mg/mL132.18 mM
Smiles
C1CC (CN (C1) C2=C3C (=CNC3=NC=C2Br) NC (=O) C4CC4) N
Molecular Formula
C17H21BrN4O
Molecular Weight
377.286
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
(R) -N- (4- (3-aminopiperidin-1-yl) -5-bromo-1H-indol-3-yl) cyclopropanecarboxamide

Chemical Information

(R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide
CAS Number1196541-47-5
PubChem CID46917793
IUPAC NameN-[4-[(3R)-3-aminopiperidin-1-yl]-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl]cyclopropanecarboxamide
Molecular FormulaC16H20BrN5O
Molecular Weight378.27
XLogP1.4
Topological Polar Surface Area87
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count4
Rotatable Bond Count3
Heavy Atom Count23
Formal Charge0
Complexity460
SMILES
C1C[C@H](CN(C1)C2=C3C(=CNC3=NC=C2Br)NC(=O)C4CC4)N
InChI
InChI=1S/C16H20BrN5O/c17-11-6-19-15-13(14(11)22-5-1-2-10(18)8-22)12(7-20-15)21-16(23)9-3-4-9/h6-7,9-10H,1-5,8,18H2,(H,19,20)(H,21,23)/t10-/m1/s1
InChIKey
BAZRWWGASYWYGB-SNVBAGLBSA-N
Chemical Structure
2D Structure
2D structure of (R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide
CAS: 1196541-47-5
CID: 46917793
Formula: C16H20BrN5O
MW: 378.27
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight378.27
XLogP31.4
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count4
Rotatable Bond Count3
Exact Mass377.08512
Monoisotopic Mass377.08512
Topological Polar Surface Area87 Ų
Heavy Atom Count23
Formal Charge0
Complexity460
Isotope Atom Count0
Defined Atom Stereocenter Count1
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

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