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Chemical Structure| 2057509-72-3 Chemical Structure| 2057509-72-3

Structure of AZD4573
CAS No.: 2057509-72-3

Chemical Structure| 2057509-72-3

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AZD4573 is a potent and highly selective CDK9 inhibitor (IC50 < 4 nM) that can be used in the research of hematological malignancies.

Synonyms: AZD4573

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Product Details of AZD4573

CAS No. :2057509-72-3
Formula : C22H28ClN5O2
M.W : 429.94
SMILES Code : O=C([C@@H]1C[C@H](NC(C)=O)CCC1)NC2=NC=C(Cl)C(C3=C(CC(C)(C)C4)N4N=C3)=C2
Synonyms :
AZD4573
MDL No. :MFCD31657407

Safety of AZD4573

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of AZD4573

Hedgehog

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
GBM42WT and GBM42R 50 nM 24 h Inhibition of GBM42WT and GBM42R cell growth and survival PMC10768977
GSC576 50 nM 24 h Inhibition of GSC576 cell growth and survival PMC10768977
GBM cells 20 nM 24 h Inhibition of GBM cell growth and survival PMC10768977
OCI-LY19 30 nM 3 h To evaluate the effect of AZD4573 on the growth of DLBCL cell lines, results showed that AZD4573 inhibited cell proliferation and induced apoptosis. PMC10061728
U-2932 30 nM 3 h To evaluate the effect of AZD4573 on the growth of DLBCL cell lines, results showed that AZD4573 inhibited cell proliferation and induced apoptosis. PMC10061728
OCI-LY3 30 nM 3 h To evaluate the effect of AZD4573 on the growth of DLBCL cell lines, results showed that AZD4573 inhibited cell proliferation and induced apoptosis. PMC10061728
VAL 30 nM 3 h To evaluate the effect of AZD4573 on the growth of DLBCL cell lines, results showed that AZD4573 inhibited cell proliferation and induced apoptosis. PMC10061728
MV4-11 cells 0, 1, 3, 10, 30, 100 nM 6, 12, 24 h Detected changes in protein levels of acetylated α-tubulin and α-tubulin, showing a concentration-dependent reduction in acetylated α-tubulin and α-tubulin levels by AZD4573. PMC11619398
MOLM-13 cells 0, 1, 3, 10, 30, 100 nM 6, 12, 24 h Detected changes in protein levels of acetylated α-tubulin and α-tubulin, showing a concentration-dependent reduction in acetylated α-tubulin and α-tubulin levels by AZD4573. PMC11619398
OCI-AML3 cells 50 nM 6 h AZD4573 decreases MCL-1 expression by inhibiting CDK9 and synergizes with venetoclax to induce apoptosis in OCI-AML3 cells. PMC8719086

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice OCI-LY3 xenograft model Intraperitoneal injection 15 mg/kg Once weekly, until tumor volume reached 20 mm in diameter or 15% of To evaluate the anti-tumor effect of AZD4573 in vivo, results showed that AZD4573 delayed tumor progression and extended survival. PMC10061728
Mice MV4-11 xenograft model Intraperitoneal injection 5 mg/kg Twice weekly for 2 days, followed by 5 days off Evaluated the anti-tumor efficacy of AZD4573 in vivo, showing significant tumor regression without notable weight loss. PMC11619398
Nude mice Subcutaneous xenograft model Intraperitoneal injection 15 mg/kg Once daily, continuous treatment Inhibition of GSC576 subcutaneous tumor xenograft growth PMC10768977

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03263637 Relapsed or Refractory Haemato... More >>logical Malignancies Including|Acute Myeloid Leukemia|Acute Lymphocytic Leukemia|Chronic Lymphocytic Leukemia|High Risk Myelodysplastic Syndrome|Chronic Myelomonocytic Leukemia|Richter's Syndrome|B-cell Non-Hodgkin Lymphoma|T-cell Non-Hodgkin Lymphoma|Small Lymphocytic Lymphoma|Multiple Myeloma Less << PHASE1 COMPLETED 2021-09-30 Research Site, Aachen, 52074, ... More >>Germany|Research Site, Bonn, 53127, Germany|Research Site, G?ttingen, 37075, Germany|Research Site, Heidelberg, 69120, Germany|Research Site, Ulm, 89081, Germany|Research Site, Amsterdam, 1105 AZ, Netherlands|Research Site, Nieuwegein, 3435 CM, Netherlands|Research Site, Cardiff, CF14 4XW, United Kingdom|Research Site, Manchester, M20 4BX, United Kingdom|Research Site, Plymouth, PL6 8DH, United Kingdom|Research Site, Southampton, S016 6YD, United Kingdom|Research Site, Sutton, SM2 5PT, United Kingdom Less <<
NCT05140382 Relapsed/Refractory Peripheral... More >> T-cell Lymphoma|Relapsed/Refractory Classical Hodgkins Lymphoma Less << PHASE2 COMPLETED 2024-02-16 Research Site, Duarte, Califor... More >>nia, 91010, United States|Research Site, Boston, Massachusetts, 02215, United States|Research Site, Hackensack, New Jersey, 07601, United States|Research Site, Houston, Texas, 77030, United States|Research Site, Salt Lake City, Utah, 84112, United States|Research Site, Seattle, Washington, 98104, United States|Research Site, Clayton, 3168, Australia|Research Site, Melbourne, 3000, Australia|Research Site, Nedlands, 6009, Australia|Research Site, Besan?on, 25000, France|Research Site, Clermont Ferrand, 63003, France|Research Site, Creteil, 94010, France|Research Site, Lille Cedex, 59037, France|Research Site, MONTPELLIER Cedex 5, 34295, France|Research Site, Bologna, 40138, Italy|Research Site, Napoli, 80131, Italy|Research Site, Seoul, 03080, Korea, Republic of|Research Site, Seoul, 03722, Korea, Republic of|Research Site, Seoul, 05505, Korea, Republic of|Research Site, Seoul, 06351, Korea, Republic of|Research Site, Lund, 221 85, Sweden|Research Site, Kaohsiung City, 83301, Taiwan|Research Site, Taichung, 40447, Taiwan|Research Site, Tainan, 70403, Taiwan|Research Site, Taipei, 100, Taiwan|Research Site, Headington, 0X3 7LJ, United Kingdom|Research Site, London, NW1 2PG, United Kingdom Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.33mL

0.47mL

0.23mL

11.63mL

2.33mL

1.16mL

23.26mL

4.65mL

2.33mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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