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Table 1 Specific CDK7 inhibitors under development

From: CDK7 in breast cancer: mechanisms of action and therapeutic potential

Name

CAS No.

Fomula

Preclinical tests

Highest

Clinical Phase

BS-181

1092443-52-1

C22H32N6

Breast cancer [70], Gastric cancer [54],

Osteosarcoma [115], Synovial sarcoma [116], Thyroid carcinoma [117],

T cell acute lymphoblastic leukemia [118]

No studies entered clinical studies yet

CT7001

1805833-75-3

C22H30N6O

Breast cancer [45], Prostate cancer [119]

Phase 1/2

LDC4297

1453834-21-3

C23H28N8O

Breast cancer [93], Pancreatic cancer [38], Lung cancer [120]

No studies entered clinical studies yet

QS1189

-

-

Mantle cell lymphoma [42]

No studies entered clinical studies yet

THZ1

1604810-83-4

C31H28ClN7O2

Breast cancer [95], Head and neck squamous cell carcinoma[121], Thyroid cancer [122], Neuroblastoma [123], Glioblastoma [124],

Gastrointestinal stromal tumours [125], Pancreatic cancer [126], Hepatocellular carcinoma [127], Gallbladder cancer [39], Cholangiocarcinoma [128], Colorectal cancer [40], Nasopharyngeal carcinoma [129], Prostate cancer [130],

Renal cell carcinoma [131], Urothelial carcinoma [132], Bladder cancer [133], Melanoma [134], Osteosarcoma [135], lymphomas [62], Leukemia [43]

No studies entered clinical studies yet

THZ2

1604810-84-5

C31H28ClN7O2

Osteosarcoma [49], Gastric cancer [136]

No studies entered clinical studies yet

YKL-5-124

1957203-01-8

C28H33N7O3

Lung cancer [53], Myeloma [137], Testicular germ cell tumors [138], Neuroblastoma [139]

No studies entered clinical studies yet

SY 5609

2417302-07-7

C23H26F3N6OP

Breast cancer [47], Ovarian cancer [10]

Phase 1

Q901

2379284-04-3

C33H36FN9O2

-

Phase 1/2

SY1365

1816989-16-8

C31H35ClN8O2

Breast cancer, Ovarian cancer, Acute myelocytic leukemia [50]

Phase 1

XL102

-

-

-

Phase 1

YKL-1-116

1957202-71-9

C34H38N8O3

Colon cancer [140]

No studies entered clinical studies yet

TY-2699a

-

-

-

Phase 1

EOC237

-

-

-

Phase 1

GTAEXS-617

-

-

-

Phase 1/2

LY3405105

2326428-25-3

C26H39N7O3

Breast cancer, Ovarian cancer, Lung cancer, Gastric cancer, Colon cancer [141]

Phase 1