2. Cell Cycle/DNA Damage
  3. Checkpoint Kinase (Chk) CDK
  4. GDC-0425 hydrochloride

GDC-0425 hydrochloride  (Synonyms: RG-7602 hydrochloride)

Cat. No.: HY-19926A
Handling Instructions Technical Support

GDC-0425 hydrochloride (RG-7602 hydrochloride) is an orally active, highly selective ChK1 inhibitor. GDC-0425 hydrochloride abrogates cell cycle arrest and inhibits genomic repair. GDC-0425 hydrochloride potently suppresses Gemcitabine (HY-17026)-induced pCDK1/2 expression. GDC-0425 hydrochloride can be used in research related to osteosarcoma, ovarian cancer, basal (triple-negative) breast cancer, and colorectal cancer.

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

GDC-0425 hydrochloride

GDC-0425 hydrochloride Chemical Structure

CAS No. : 1778671-05-8

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GDC-0425 hydrochloride Related Antibodies

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Chk1 Chk2 BUBR1

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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Description

GDC-0425 hydrochloride (RG-7602 hydrochloride) is an orally active, highly selective ChK1 inhibitor. GDC-0425 hydrochloride abrogates cell cycle arrest and inhibits genomic repair. GDC-0425 hydrochloride potently suppresses Gemcitabine (HY-17026)-induced pCDK1/2 expression. GDC-0425 hydrochloride can be used in research related to osteosarcoma, ovarian cancer, basal (triple-negative) breast cancer, and colorectal cancer.

IC50 & Target[1][2]

Chk1

 

CDK2

 

CDK1

 

In Vitro

GDC-0425 (3 μM; 48 h) alters the cell cycle distribution of both sensitive and resistant cancer cell lines, but induces the formation of apoptotic sub-G0/G1 cell populations only in sensitive osteosarcoma, ovarian cancer and breast cancer cell lines[3].
GDC-0425 (3 μM; 24 h) induces hyperphosphorylation of Chk1 in U-2 OS cells[3].

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

GDC-0425 hydrochloride Related Antibodies

Cell Cycle Analysis[3]

Cell Line: cancer cell lines (143B PML BK TK, COV413B, HCC70, SW1353, OVISE, HCC1419)
Concentration: 3 μM
Incubation Time: 48 h
Result: Reduced the S phase population and increased the G0/G1 phase population in both sensitive and resistant cell lines (except SW1353).
Caused a large increase in the sub-G0/G1 population (apoptotic cells) only in sensitive cell lines.
In Vivo

GDC-0425 (hydrochloride) (50 mg/kg; p.o.; single dose; administered 16 hours after gemcitabine) potently inhibits gemcitabine-induced pCDK1/2 expression, indicating Chk1 checkpoint abrogation in TP53G12C mutant HT-29 colorectal xenografts[2].
GDC-0425 (75 mg/kg; p.o.; 3 times per week; 15 days) alone partially suppresses osteosarcoma tumor growth, while combination with gemcitabine induces significant tumor regression with good tolerability in NCr nude mice[3].
GDC-0425 (50-75 mg/kg; p.o.; 3 times per week) alone partially suppresses triple-negative breast cancer (HCC1806) tumor growth, while combinations with gemcitabine induce significant tumor regression with good tolerability in NCr nude mice[3].
GDC-0425 (50-75 mg/kg; p.o.; 3 times per week) alone partially suppresses triple-negative breast cancer (HCC70) tumor growth, while combinations with gemcitabine induce significant tumor regression in NCr nude mice[3].

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

Animal Model: NCR nude (female; subcutaneous xenograft of TP53 mutant HT-29 colorectal cancer cells, tumors grown to 300-450 mm3)[2]
Dosage: 50 mg/kg
Administration: p.o.; single dose; administered 16 hours after gemcitabine
Result: Caused marked inhibition of gemcitabine-induced pCDK1/2 expression.
Showed little effect on pCDK1/2 expression when administered alone.
Left Ki-67 expression in surviving tumor cells relatively consistent across treatment groups.
Animal Model: NCr nude mice[3]
Dosage: 75 mg/kg (single-agent); 75 mg/kg (in combination with gemcitabine 120 mg/kg)
Administration: p.o.; 3 times per week; i.p. (weekly, gemcitabine)
Result: Caused partial suppression of tumor growth (single-agent).
Induced significant tumor regression, with tumor volumes remaining near baseline over the 15-day treatment period (in combination with gemcitabine).
Did not cause significant body weight loss (in combination with gemcitabine).
Animal Model: NCr nude mice[3]
Dosage: 50 mg/kg (single-agent); 75 mg/kg (single-agent); 50 mg/kg (in combination with gemcitabine 120 mg/kg); 75 mg/kg (in combination with gemcitabine 120 mg/kg)
Administration: p.o.; 3 times per week; i.p. (weekly, gemcitabine)
Result: Caused partial suppression of tumor growth at 50 mg/kg and 75 mg/kg (single-agent).
Induced significant tumor regression, with tumor volumes remaining near baseline over the treatment period (in combination with gemcitabine at both doses).
Did not cause significant body weight loss (in combination with gemcitabine).\nCaused partial suppression of tumor growth at 50 mg/kg and 75 mg/kg (single-agent).
Induced significant tumor regression, with tumor volumes remaining near baseline over the treatment period (in combination with gemcitabine at both doses).
Molecular Weight

394.30

Formula

C18H21Cl2N5O
CAS No.
SMILES

N#CC1=NC=C2NC3=C(C2=C1OC4CCN(CC4)CC)C=CC=N3.Cl.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GDC-0425 hydrochloride Related Classifications

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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:

GDC-04251778671-05-8RG-7602GDC0425GDC 0425RG7602RG 7602Checkpoint Kinase (Chk)CDKCyclin dependent kinaseCheckpoint kinase 1ChK1HT-29 colorectal xenograftsDNA damageHCC1806HCC70ovarian cancerosteosarcomaNCr nude micetriple-negative breast cancerInhibitorinhibitorinhibit

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