For research use only.

Catalog No.S8253 Synonyms: SRA737, PNT-737

5 publications

CCT245737 Chemical Structure

CAS No. 1489389-18-5

CCT245737 (SRA737, PNT-737) is an orally active CHK1 inhibitor with The IC50 of 1.4 nM. It exhibits >1,000-fold selectivity against CHK2 and CDK1.

Selleck's CCT245737 has been cited by 5 publications

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Biological Activity

Description CCT245737 (SRA737, PNT-737) is an orally active CHK1 inhibitor with The IC50 of 1.4 nM. It exhibits >1,000-fold selectivity against CHK2 and CDK1.
Chk1 [1]
(Cell-free assay)
1.4 nM
In vitro

CCT245737 is a potent inhibitor of recombinant human CHK1 with IC50 of 1.4±0.3 nM (mean±SD, n = 3, EZ Reader II assay). There is > 1,000-fold selectivity for CHK1 versus the functionally important kinases CDK1 and CHK2 (IC50=1.26-2.44 and 9.03 μM, respectively), and at least a 90-fold selectivity against cross-reacting kinases such as ERK8, PKD1, RSK1 and 2. CCT245737 potently inhibits cellular CHK1 activity (IC50 30-220nM) and enhances gemcitabine and SN38 cytotoxicity in multiple human tumor cell lines and human tumor xenograft models. It can abrogate an etoposide-induced G2/M arrest. CCT245737 has high cell permeability, as measured by transport across a CaCo2 cell monolayer[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 cells NEXSeWhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M1L0WVczKGi{cx?= NIPYV4dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjFT|I6OyClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRUKGG|c3H5MEBIUTVyPUGuN|g4|ryPLh?= M1rlOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Nki0PFk1Lz5{OU[4OFg6PDxxYU6=
HT-29 cells MYnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NUfj[o4zPzJiaILz MoPnRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVD2yPUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTTJIF{e2G7LDDHTVUxRTlwMkKz{txONg>? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTZ6NEi5OEc,Ojl4OES4PVQ9N2F-

... Click to View More Cell Line Experimental Data

In vivo Mouse oral bioavailability is complete (100%) with extensive tumor exposure. CCT245737 shows significant single-agent activity against a MYC-driven mouse model of B-cell lymphoma. An i.v. dose of 10mg/kg CCT245737 into BALB/c mice gives a peak plasma concentration of 4μmol/L, with a half-life of 2.86h, an AUC0-∞ of 9.96μmol.h/L, a plasma clearance of 2.1L/h/kg and a large volume of distribution (0.19L). The equivalent oral dose gave an almost identical profile with an AUC0-∞ of 10.4μmol.h/L showing complete oral bioavailability (F = 105%). In a word, CCT245737 shows complete oral bioavailability with linear pharmacokinetics and high tumor/plasma ratios consistent with extensive tumor exposure. Adequate CCT245737 tumor drug exposure takes a significant antitumor activity[1].


Cell Research:[1]
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  • Cell lines: The colon tumor cell lines HT29 and SW620, the pancreatic cancer cell line MiaPaCa-2 and the non-small cell lung cancer Calu6 cell line
  • Concentrations: --
  • Incubation Time: 96 h
  • Method: Cytotoxicity is determined as the drug concentration that gave 50% inhibition of tumor cell proliferation (GI50) using a 96h (i.e. 4-doublings) Sulforhodamine B (SRB) assay. Inhibition of intracellular CHK1 activity is measured using a cell based ELISA for the abrogation of an etoposide induced G2 checkpoint (mitosis induction assay, MIA).
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: BALB/c mice
  • Dosages: 10mg/kg(i.v.); 150mg/kg(p.o.)
  • Administration: i.v. or p.o. administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 75 mg/mL warmed (197.71 mM)
Ethanol 9 mg/mL warmed (23.72 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 379.34


CAS No. 1489389-18-5
Storage powder
in solvent
Synonyms SRA737, PNT-737
Smiles C1COC(CN1)CNC2=CC(=NC=C2C(F)(F)F)NC3=NC=C(N=C3)C#N

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02797964 Completed Drug: SRA737 Advanced Solid Tumors or Non-Hodgkin''s Lymphoma (NHL) Sierra Oncology Inc. July 2016 Phase 1|Phase 2
NCT02797977 Completed Drug: SRA737 gemcitabine cisplatin|Drug: SRA737 gemcitabine Advanced Solid Tumors Sierra Oncology Inc. July 2016 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID